2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Abstract

Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2′;6′,2″]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines. © 2011 Elsevier Inc. All rights reserved.