Synthesis and antitumor activity of bithienyl-pyrimidine derivatives with electrostatic binding side chains

YM Chou, MC Lai, TM Hwang, CW Ong

Index: Chou, Yi-Meen; Lai, Ming Chih; Hwang, Tsai-Mian; Ong, Chi Wi Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 18 p. 2643 - 2646

Full Text: HTML

Citation Number: 4

Abstract

A series of bithienyl-pyrimidines having cationic side chain have been developed as antitumor agents. This work illustrates the overwhelming importance of the bithienyl unit for efficient DNA binding. The X-ray structure of 4-(2′, 2 ″-thien-5-yl)-2-chloropyrimidine was obtained for postulating the conformation of the bithienyl-pyrimidine moiety.