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

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

  • Bioorg Med Chem Lett. 2001 Oct 8;11(19):2659-62. doi: 10.1016/s0960-894x(01)00531-5.
L X Zhao 1,  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
Affiliations

Affiliation

  • 1 College of Pharmacy, Yeungnam University, Kyongsan 712-749, South Korea.
PMID: 11551772 DOI: 10.1016/s0960-894x(01)00531-5
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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