Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase

…, E Tloušt'ová, K Horská, M Masojídková…

Index: Nencka, Radim; Votruba, Ivan; Hrebabecky, Hubert; Jansa, Petr; Tloust'ova, Eva; Horska, Kveta; Masojidkova, Milena; Holy, Antonin Journal of Medicinal Chemistry, 2007 , vol. 50, # 24 p. 6016 - 6023

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Citation Number: 31

Abstract

Thymidine phosphorylase plays an important role in angiogenesis, which is an attractive target for therapy of cancer and other diseases. In our continuous effort to develop novel inhibitors of thymidine phosphorylase, we have discovered that 6-halouracils substituted at position C5 by certain hydrophobic groups exhibit significant inhibitory activity against this enzyme. The most potent compounds bear a five-or six-membered cyclic substituent ...