Discovery of mixed type thymidine phosphorylase inhibitors endowed with antiangiogenic properties: Synthesis, pharmacological evaluation and molecular docking …

…, P kumar Ojha, BJ Tan, L Sun, AV Dolzhenko…

Index: Bera, Hriday; Ojha, Probir Kumar; Tan, Bee Jen; Sun, Lingyi; Dolzhenko, Anton V.; Chui, Wai-Keung; Chiu, Gigi Ngar Chee European Journal of Medicinal Chemistry, 2014 , vol. 78, p. 294 - 303

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Citation Number: 11

Abstract

Abstract In our drug discovery program, a series of 2-thioxo-pyrazolo [1, 5-a][1, 3, 5] triazin-4- ones were designed, synthesized and evaluated for their TP inhibitory potential. All the synthesized analogues conferred a varying degree of TP inhibitory activity, comparable or better than positive control, 7-deazaxanthine (7-DX, 2)(IC 50 value= 42.63 μM). A systematic approach to the lead optimization identified compounds 3c and 4a as the most promising ...