Structure–activity relationship of 2, 4, 5-trioxoimidazolidines as inhibitors of thymidine phosphorylase

M Rajabi, D Mansell, S Freeman, RA Bryce

Index: Rajabi, Mehdi; Mansell, David; Freeman, Sally; Bryce, Richard A. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1165 - 1171

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Citation Number: 8

Abstract

Novel non-nucleobase-derived inhibitors of the angiogenic enzyme, thymidine phosphorylase, have been identified using molecular modelling, synthesis and biological evaluation. These inhibitors are 2, 4, 5-trioxoimidazolidines bearing N-(substituted) phenylalkyl groups, together with, in most cases, N′-(CH2) n-carboxylic acid, ester or amide side chains. The best compound from this series is 3-(2, 4, 5-trioxo-3-phenylethyl- ...