Synthesis and antitumor activity of bithienyl-pyrimidine derivatives with electrostatic binding side chains.
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.
Chou
Y M
YM
Department of Chemistry, National Sun Yat Sen University, Kaoshiung, Taiwan.
Lai
M C
MC
Hwang
T M
TM
Ong
C W
CW
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D055672:Static Electricity; D014407:Tumor Cells, Cultured; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D011743:Pyrimidines