Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives |
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| Authors: | Zhao L X Kim T S Ahn S H Kim T H Kim E K Cho W J Choi H Lee C S Kim J A Jeong T C Chang C J Lee E S |
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| Institution: | College of Pharmacy, Yeungnam University, Kyongsan 712-749, South Korea. |
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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. |
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