Protein structure-based design, synthesis, and biological evaluation of 5-thia-2, 6-diamino-4 (3 H)-oxopyrimidines: Potent inhibitors of glycinamide ribonucleotide …

…, WH Romines, T Boritzki, SA Margosiak…

Index: Varney, Michael D.; Palmer, Cindy L.; Romines III, William H.; Boritzki, Theodore; Margosiak, Stephen A.; Almassy, Robert; Janson, Cheryl A.; Bartlett, Charlotte; Howland, Eleanor J.; Ferre, Rosanne Journal of Medicinal Chemistry, 1997 , vol. 40, # 16 p. 2502 - 2524

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Citation Number: 42

Abstract

The design, synthesis, biochemical, and biological evaluation of a novel series of 5-thia-2, 6- diamino-4 (3 H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo-2, 6-diamino-4 (3 H)-pyrimidinone, 20. The bicyclic compounds were ...