Target Validation Information
Target ID T13260
Target Name Cytochrome P450 19
Target Type
Successful
Drug Potency against Target 1-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 150 nM
5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one Drug Info IC50 = 2100 nM [535139]
1-(4-nitro-2-phenoxybenzyl)-1H-imidazole Drug Info IC50 = 11.45 nM
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Drug Info IC50 = 390 nM
MDL-18962 Drug Info IC50 = 56.2 nM [534514]
2,4-Dimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 11140 nM
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Drug Info IC50 = 40 nM [535139]
4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one Drug Info IC50 = 16.5 nM
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 940 nM [535139]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Drug Info IC50 = 2440 nM [531085]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 3070 nM [531085]
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 663 nM [531085]
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 814 nM [528109]
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Drug Info IC50 = 5.59 nM
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Drug Info IC50 = 210 nM [530712]
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 590 nM
3,4,5-Trimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 16420 nM
1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone Drug Info IC50 = 1840 nM
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 1787 nM [528109]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1550 nM [527456]
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 180 nM [527456]
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Drug Info IC50 = 15 nM [529291]
1-(2-phenoxybenzyl)-1H-imidazole Drug Info IC50 = 389.2 nM
2,3,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 2280 nM
3-Amino-4'-amino-trans-stilbene Drug Info IC50 = 7470 nM
2,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 760 nM
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4720 nM [527456]
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 9740 nM [527456]
4-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 2740 nM [527456]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3400 nM [527456]
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1280 nM [527456]
1-Naphthalen-2-yl-1H-imidazole Drug Info IC50 = 2821 nM [527801]
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Drug Info IC50 = 790 nM [527456]
4-(2,2-Diphenyl-vinyl)-pyridine Drug Info IC50 = 100 nM [527456]
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 7680 nM [527456]
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 130 nM [527456]
3-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 4810 nM [527456]
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 12630 nM [527456]
4-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 6700 nM [527456]
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 5430 nM [527456]
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 6045 nM [528109]
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3720 nM [527456]
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1990 nM [527456]
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 6360 nM [527456]
3-(naphthalen-2-yl)pyridine Drug Info IC50 = 5700 nM [529834]
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 2540 nM [527456]
3-(3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 4073 nM [528109]
N-[2-(4'-Nitrophenyl)ethyl]-imidazole Drug Info IC50 = 160 nM [530867]
ALPHA-NAPHTHOFLAVONE Drug Info IC50 = 70 nM [530867]
3,5-Diacetoxy-4'-amino-trans-stilbene Drug Info IC50 = 2940 nM
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Drug Info IC50 = 90 nM [527222]
3-(6-methoxynaphthalen-2-yl)pyridine Drug Info IC50 = 600 nM [529834]
3-(6-Ethoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 6638 nM [527801]
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 9107 nM [527801]
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1710 nM [527456]
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Drug Info IC50 = 2830 nM [531085]
5-Indan-(1E)-ylidenemethyl-1H-imidazole Drug Info IC50 = 955 nM [527475]
4-(1-Imidazol-1-yl-vinyl)-benzonitrile Drug Info IC50 = 0.7 nM [534057]
7-((1H-imidazol-1-yl)methyl)isoquinoline Drug Info IC50 = 1380 nM [529860]
3,5-Diamino-4'-amino-trans-stilbene Drug Info IC50 = 8510 nM
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2510 nM [528035]
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 910 nM [528035]
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Drug Info IC50 = 129 nM [527801]
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 27 nM [527475]
5-Indan-(1Z)-ylidenemethyl-1H-imidazole Drug Info IC50 = 130 nM [527475]
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 1507 nM [528109]
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7830 nM [527456]
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 230 nM [527456]
2,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 1820 nM
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Drug Info IC50 = 205 nM [525448]
7-hydroxy-2-phenylchroman-4-one Drug Info IC50 = 3800 nM [529180]
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 1860 nM [528848]
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3960 nM [527456]
5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole Drug Info IC50 = 4830 nM [527456]
3-(2,2-Diphenyl-vinyl)-pyridine Drug Info IC50 = 3630 nM [527456]
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4260 nM [527456]
3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4060 nM [527456]
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Drug Info IC50 = 4330 nM [527456]
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 4100 nM [528327]
1-(9H-fluoren-9-yl)-1H-imidazole Drug Info IC50 = 2850 nM [529860]
3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 4600 nM [527456]
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1810 nM [527456]
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7080 nM [527456]
3-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 2040 nM [527456]
NSC-368272 Drug Info Ki = 5.6 nM [529860]
3-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 3550 nM [527456]
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3930 nM [527456]
5-(2-(1H-imidazol-1-yl)ethyl)quinoline Drug Info IC50 = 350 nM [529860]
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4310 nM [527456]
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2490 nM [527456]
4-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 12730 nM [527456]
NSC-369087 Drug Info IC50 = 55 nM [529860]
3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione Drug Info IC50 = 8400 nM [533480]
6-Imidazol-1-yl-isoquinoline Drug Info IC50 = 3060 nM [529860]
Letrozole Drug Info IC50 = 0.8 nM [552393]
2-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 7900 nM
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2670 nM [528035]
4-(3,4,5-Trimethoxyphenethyl)aniline Drug Info IC50 = 2790 nM
4-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 17 nM
Gamma-mangostin Drug Info IC50 = 4970 nM [529538]
NSC-19028 Drug Info IC50 = 8 nM [530867]
3,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 14510 nM
NSC-93358 Drug Info Ki = 266 nM [530190]
NSC-613604 Drug Info Ki = 385 nM [530190]
YM-511 Drug Info IC50 = 0.5 nM [526667]
ANDROSTENEDIONE Drug Info Ki = 20 nM [533863]
MR-16089 Drug Info IC50 = 40 nM [530867]
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Drug Info IC50 = 2 nM [530867]
LIAROZOLE Drug Info IC50 = 5 nM [530867]
MR-20492 Drug Info IC50 = 200 nM [530867]
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Drug Info IC50 = 1 nM [530867]
NSC-94891 Drug Info IC50 = 9800 nM [530190]
NSC-356781 Drug Info IC50 = 2100 nM [529860]
LUDARTIN Drug Info IC50 = 55 nM [530867]
APIGENIN Drug Info IC50 = 900 nM [530867]
CHRYSIN Drug Info IC50 = 1 nM [530867]
NSC-12999 Drug Info Ki = 25.5 nM [529860]
NSC-131736 Drug Info IC50 = 1400 nM [529860]
DEHYDROLEUCODIN Drug Info IC50 = 15 nM [530867]
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 680 nM [529860]
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Drug Info IC50 = 3560 nM [529860]
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Drug Info IC50 = 100 nM [529860]
NSC-289311 Drug Info Ki = 6.5 nM [529860]
NSC-368280 Drug Info Ki = 1.9 nM [529860]
4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info IC50 = 760 nM [529860]
5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline Drug Info IC50 = 170 nM [529860]
ISOLICOFLAVONOL Drug Info IC50 = 100 nM [526180]
CGS-18320B Drug Info IC50 = 3 nM [530867]
(2S)-5,7,2',4'-tetrahydroxyflavanone Drug Info IC50 = 2200 nM [526180]
MORACHALCONE A Drug Info IC50 = 4600 nM [526180]
NSC-625409 Drug Info Ki = 52.7 nM [529860]
2,3-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 980 nM
4-(3,4-Dimethoxyphenethyl)aniline Drug Info IC50 = 670 nM
ALBANOL A Drug Info IC50 = 7500 nM [526180]
1-(3-(4-fluorophenyl)propyl)-1H-imidazole Drug Info IC50 = 310 nM [530867]
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Drug Info IC50 = 160 nM [530867]
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Drug Info IC50 = 74 nM [530867]
BIOCHANIN Drug Info IC50 = 10.2 nM [530867]
2-(4-hydroxyphenyl)-7-methoxychroman-4-one Drug Info IC50 = 3700 nM [529180]
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 770 nM [527456]
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2800 nM [527456]
NSC-75308 Drug Info IC50 = 5600 nM [529860]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Drug Info IC50 = 7450 nM [527456]
3-(imidazolylmethyl)flavone Drug Info IC50 = 71 nM [528327]
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Drug Info IC50 = 470 nM [528327]
3-(imidazolylmethyl)-4'-methoxyflavone Drug Info IC50 = 80 nM [528327]
(2S)-euchrenone a7 Drug Info IC50 = 3400 nM [526180]
10-EPI-8-DEOXY-CUMAMBRIN B Drug Info IC50 = 7 nM [530867]
NSC-666292 Drug Info Ki = 33.4 nM [529860]
4-(3,5-Dimethoxyphenethyl)benzenamine Drug Info IC50 = 2760 nM
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 100 nM [527475]
MR-20496 Drug Info Ki = 10.3 nM [534789]
MR-20494 Drug Info IC50 = 110 nM [530867]
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 2100 nM [529860]
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Drug Info IC50 = 970 nM [535139]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info IC50 = 8000 nM [529180]
9-Hydroxy-7,8-benzoflavone Drug Info IC50 = 20 nM [530867]
2-(3-hydroxyphenyl)-7-methoxychroman-4-one Drug Info IC50 = 3500 nM [529180]
8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one Drug Info IC50 = 1100 nM [535139]
7,4'-Dihydroxyflavone Drug Info IC50 = 2 nM [530867]
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Drug Info IC50 = 2693 nM [531085]
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 89 nM [535139]
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Drug Info IC50 = 3700 nM [535139]
NSC-94258 Drug Info IC50 = 30.5 nM [530867]
NARINGENIN Drug Info IC50 = 2.9 nM [530867]
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Drug Info IC50 = 4000 nM [529860]
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 280 nM [527456]
NSC-683634 Drug Info Ki = 15.1 nM [529860]
NSC-356483 Drug Info IC50 = 3100 nM [529860]
3-(imidazolylmethyl)-4'-nitroflavone Drug Info IC50 = 45 nM [528327]
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3680 nM [527456]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 800 nM [527456]
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 7370 nM [527456]
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 4050 nM [527456]
ANDROSTENEDONE Drug Info Ki = 120 nM [533387]
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [533480]
Isogemichalcone C Drug Info IC50 = 7100 nM [526180]
4-((1H-imidazol-1-yl)methyl)benzonitrile Drug Info IC50 = 15 nM [529291]
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 3551 nM [528109]
2,3,4-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 3570 nM
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Drug Info IC50 = 1900 nM
NSC-122427 Drug Info IC50 = 15500 nM [530190]
3-Nitro-4'-nitro-trans-stilbene Drug Info IC50 = 8330 nM
3,4'-(Ethane-1,2-diyl)dibenzenamine Drug Info IC50 = 3210 nM
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [533480]
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Drug Info IC50 = 430 nM [527222]
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Drug Info IC50 = 1200 nM [529684]
Anastrozole Drug Info IC50 = 15 nM [552393]
Exemestane Drug Info IC50 = 5 nM [552393]
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Drug Info IC50 = 10200 nM [533480]
GARCINONE D Drug Info IC50 = 5200 nM [529538]
(2S)-abyssinone II Drug Info IC50 = 400 nM [526180]
Rogletimide Drug Info Ki = 14000 nM [533470]
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 5570 nM [527456]
7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one Drug Info IC50 = 3400 nM [529180]
FADROZOLE Drug Info IC50 = 17 nM [527856]
Docosapentaenoic acid Drug Info IC50 = 16800 nM [528166]
3-Methoxyl-4'-amino-trans-stilbene Drug Info IC50 = 3080 nM
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 1805 nM [527801]
COUMATE Drug Info IC50 = 300 nM [530712]
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Drug Info IC50 = 950 nM [529684]
4'-cyano-3-(imidazolylmethyl)flavone Drug Info IC50 = 69 nM [528327]
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 1800 nM [528327]
4'-bromo-3-(imidazolylmethyl)flavone Drug Info IC50 = 440 nM [528327]
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Drug Info IC50 = 190 nM
MONODICTYOCHROMONE B Drug Info IC50 = 16500 nM [529759]
Aminoglutethimide Drug Info IC50 = 18500 nM [552532]
4-Imidazol-1-ylmethylthioxanthen-9-one Drug Info IC50 = 3.98 nM
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Drug Info IC50 = 53 nM
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 900 nM
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Drug Info IC50 = 4300 nM [529180]
Broussoflavonol F Drug Info IC50 = 9700 nM [526180]
4-Imidazol-1-yl-2-phenyl-chroman-7-ol Drug Info IC50 = 40 nM [527222]
2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one Drug Info IC50 = 770 nM [527565]
LIQUIRTIGENIN Drug Info IC50 = 340 nM [529679]
GOSSYPETIN Drug Info IC50 = 11000 nM [529679]
3,5-Dihydroxyl-4'-amino-trans-stilbene Drug Info IC50 = 5000 nM
Action against Disease Model Testolactone Potency and selectivity of aromatase inhibition are parameters which ultimately influence the therapeutic efficacy of aromatase inhibitors. This report describes an in vitro model which allows an assessment of the selectivity with which aromatase inhibitors inhibit estrogen biosynthesis. Estrogen production was stimulated by incubating adult female hamster ovarian tissue with ovine LH. The production rates of estrogens (E), testosterone (T) and progesterone (P) were determined using radioimmunoassays to measure the amount of these steroids released into the incubation medi uM over a 4-hour incubation period. The selectivity of aromatase inhibition was assessed by determining the IC50S with which each inhibitor inhibited the production of E (end product), T (immediateprecursor of E) and P (early precursor of E). Selectivity was studied for each of the 4 aromatase inhibitors, CGS 16949A (a new non-steroidal compound), 4-OH-androstenedione, aminoglutethimide and testolactone. CGS 16949A was the most potent of the four, followed by 4-OH-androstenedione, aminoglutethimide and testolactone. As far as selectivity was concerned, both CGS 16949A and 4-OH-androstenedione selectively inhibited aromatase judging from the IC50s for E and P production (CGS 16949A: IC50 for E & P = 0.03 & 160 microM, resp.; 4-OH-androstenedione: IC50 for E & P = 0.88 & greater than or equal to 330 microM, resp.). Aminoglutethimide was the least selective inhibitor of aromatase (IC50 for E & P = 13 & 60 microM, resp.). For testolactone, the least potent of the four (IC50 for E = 130microM), no conclusive data were obtained concerning the selectivity of aromatase inhibition. Thus a simple, effective and reproducible method is described for assessing the selectivity with which aromatase inhibitors inhibit aromatase. [553113] Drug Info
References
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 534514J Med Chem. 1997 Sep 26;40(20):3263-70.6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 530712J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529291J Med Chem. 1991 Feb;34(2):725-36.Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Ref 553113An in vitro method to determine the selective inhibition of estrogen biosynthesis by aromatase inhibitors. J Steroid Biochem. 1989 Jul;33(1):125-31.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529834J Med Chem. 2008 Dec 25;51(24):8077-87.In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 527222Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8.Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Ref 529834J Med Chem. 2008 Dec 25;51(24):8077-87.In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 527475J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Ref 534057J Med Chem. 1993 May 14;36(10):1393-400.Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 528035J Med Chem. 2006 Feb 23;49(4):1413-9.Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
Ref 528035J Med Chem. 2006 Feb 23;49(4):1413-9.Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527475J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Ref 527475J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 525448Bioorg Med Chem Lett. 1999 Feb 8;9(3):333-6.New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 528848J Med Chem. 2007 Jun 14;50(12):2799-806. Epub 2007 May 19.Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 533480J Med Chem. 1986 Apr;29(4):520-3.Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 552393The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003 Oct;87(1):35-45.
Ref 528035J Med Chem. 2006 Feb 23;49(4):1413-9.Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
Ref 529538J Nat Prod. 2008 Jul;71(7):1161-6. Epub 2008 Jun 18.Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530190Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Ref 530190Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Ref 526667J Med Chem. 2003 Jul 17;46(15):3193-6.First dual aromatase-steroid sulfatase inhibitors.
Ref 533863J Med Chem. 1994 Jul 8;37(14):2198-205.Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530190Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527475J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Ref 534789Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4.Design and synthesis of a new type of non steroidal human aromatase inhibitors.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 535139A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 530867Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 533387J Med Chem. 1989 Mar;32(3):651-8.Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione.
Ref 533480J Med Chem. 1986 Apr;29(4):520-3.Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 529291J Med Chem. 1991 Feb;34(2):725-36.Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 530190Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Ref 533480J Med Chem. 1986 Apr;29(4):520-3.Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Ref 527222Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8.Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Ref 529684Bioorg Med Chem. 2008 Sep 15;16(18):8349-58. Epub 2008 Aug 26.CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Ref 552393The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003 Oct;87(1):35-45.
Ref 552393The pharmacology of letrozole. J Steroid Biochem Mol Biol. 2003 Oct;87(1):35-45.
Ref 533480J Med Chem. 1986 Apr;29(4):520-3.Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Ref 529538J Nat Prod. 2008 Jul;71(7):1161-6. Epub 2008 Jun 18.Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 533470J Med Chem. 1987 Sep;30(9):1550-4.Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 527856J Med Chem. 2005 Nov 17;48(23):7282-9.Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.
Ref 528166J Nat Prod. 2006 Apr;69(4):700-3.Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 530712J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Ref 529684Bioorg Med Chem. 2008 Sep 15;16(18):8349-58. Epub 2008 Aug 26.CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 529759J Nat Prod. 2008 Dec 1;71(11):1793-1799. Epub 2008 Oct 21.Monodictyochromes A and B, Dimeric Xanthone Derivatives from the Marine Algicolous Fungus Monodictys putredinis.
Ref 552532Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase. J Enzyme Inhib Med Chem. 2005 Apr;20(2):135-41.
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 527222Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8.Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Ref 527565Bioorg Med Chem. 2005 Jun 2;13(12):4063-70. Epub 2005 Apr 25.Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Ref 529679Bioorg Med Chem. 2008 Sep 15;16(18):8466-70. Epub 2008 Aug 19.Screening of herbal constituents for aromatase inhibitory activity.
Ref 529679Bioorg Med Chem. 2008 Sep 15;16(18):8466-70. Epub 2008 Aug 19.Screening of herbal constituents for aromatase inhibitory activity.

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