Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives.

L X Zhao, T S Kim, S H Ahn, T H Kim, E K Kim, W J Cho, H Choi, C S Lee, J A Kim, T C Jeong, C J Chang, E S Lee

Index: Bioorg. Med. Chem. Lett. 11(19) , 2659-62, (2001)

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Abstract

For the development of new anticancer agents, 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2':6',2"-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives were potent topoisomerase I inhibitors.