Synthesis and in vitro Evaluation of 1, 2, 4??Triazolo [1, 5??a][1, 3, 5] triazine Derivatives as Thymidine Phosphorylase Inhibitors

…, AV Dolzhenko, L Sun, S Dutta Gupta…

Index: Bera, Hriday; Dolzhenko, Anton V.; Sun, Lingyi; Dutta Gupta, Sayan; Chui, Wai-Keung Chemical Biology and Drug Design, 2013 , vol. 82, # 3 p. 351 - 360

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Citation Number: 10

Abstract

In our lead finding program, a series of 1, 2, 4-triazolo [1, 5-a][1, 3, 5] triazine derivatives were synthesized, and their in vitro thymidine phosphorylase inhibitory potential was explored. Among the different derivatives, compounds having keto group (C= O) at C7 and thioketo group (C= S) at C5 positions showed varying degrees of TP inhibitory activity comparable with positive control, 7-deazaxanthine(7-DX, 2)(IC50 value= 42.63 lM). ...