Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 1: discovery of novel orally active inhibitors of human thymidine phosphorylase

…, J Yamashita, Y Tada, Y Yamada, M Fukushima…

Index: Yano, Shingo; Kazuno, Hideki; Suzuki, Norihiko; Emura, Tomohiro; Wierzba, Konstanty; Yamashita, Jun-Ichi; Tada, Yukio; Yamada, Yuji; Fukushima, Masakazu; Asao, Tetsuji Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 13 p. 3431 - 3441

Full Text: HTML

Citation Number: 31

Abstract

A series of novel 6-methylene-bridged uracil derivatives have been prepared as inhibitors of human thymidine phosphorylase (TP). To enhance the in vivo antitumor activity of fluorinated pyrimidine 2′-deoxyribonucleosides such as 2′-deoxy-5-(trifluoromethyl) uridine (F3dThd), a potent TP inhibitor preventing their degradation to an inactive compound, has become a target of medicinal chemistry. We present here the synthesis ...