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
  • 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.