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

Article abstract of DOI:10.1016/S0960-894X(99)00441-2

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.