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

For the development of new anticancer agents, 2,2':6',2 "-, 2,2':6'.3 "- an d 2,2':6',4 " -terpyridine derivatives were designed and evaluated for thei r topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure activity relationship studies indicated that 2,2':6',2 " -terpyridine deri vatives were highly cytotoxic toward several human tumor cell lines, wherea s 2,2':6',3 "- and 2,2':6',4 " -terpyridine derivatives were potent topoiso merase I inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.