Synthesis and evaluation of multisubstrate bicyclic pyrimidine nucleoside inhibitors of human thymidine phosphorylase

…, RJ Ternansky, DE Shaw, B Ganem, Y Li…

Index: Allan, Amy L.; Gladstone, Patricia L.; Price, Melissa L. P.; Hopkins, Stephanie A.; Juarez, Jose C.; Donate, Fernando; Ternansky, Robert J.; Shaw, David E.; Ganem, Bruce; Li, Yingbo; Wang, Weiru; Ealick, Steven Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7807 - 7815

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Citation Number: 23

Abstract

A series of novel, multisubstrate, bicyclic pyrimidine nucleoside inhibitors of human thymidine phosphorylase (TP) is described. Thymidine phosphorylase has been implicated in angiogenesis and plays a significant role in tumor progression and metastasis. The presence and orientation of the phosphonate moiety (acting as a phosphate mimic) in these derivatives were critical for inhibitory activity. The most active compounds possessed a ...