Target Validation Information
TTD ID T52227
Target Name Candida Thymidylate synthase (Candi TMP1)
Type of Target
Successful
Drug Potency against Target Fluorouracil Drug Info IC50 = 899 nM [6]
Drug Info IC50 = 100 nM [1]
Drug Info IC50 = 19 nM [3]
1,3-propanediphosphonic acid Drug Info Ki = 2700 nM [4]
3-Amino-5,6-dihydro-2H-benzo[f]quinazolin-1-one Drug Info Ki = 7000 nM [5]
3-Methyl-2H-benzo[f]quinazolin-1-one Drug Info Ki = 5400 nM [5]
PREMETREXED Drug Info IC50 = 9500 nM [2]
References
REF 1 Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methy... J Med Chem. 2005 Nov 17;48(23):7215-22.
REF 2 Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical ... J Med Chem. 2006 Feb 9;49(3):1055-65.
REF 3 Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual th... J Med Chem. 2009 Aug 13;52(15):4892-902.
REF 4 Novel approaches for targeting thymidylate synthase to overcome the resistance and toxicity of anticancer drugs. J Med Chem. 2010 Sep 23;53(18):6539-49.
REF 5 Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related de... J Med Chem. 1993 Oct 29;36(22):3464-71.
REF 6 Mechanism of action of key enzymes associated with cancer propagation and their inhibition by various chemotherapeutic agents. Mini Rev Med Chem. 2008 Apr;8(4):388-98.

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