Design, synthesis and antitumor activity of 3-substituted quinolone derivatives (I)

A series of quinolone derivatives containing benzimidazole, benzoxazole or benzothiazole ring were synthesized. The cytotoxicity of 12 new compounds was evaluated in KB, Bel7402, A2780 and HT-29 cell lines. Most of synthesized compounds showed moderate inhibitory activity against cancer cells. The inhibitory activities of 6k, against KB and A2780 tumor cells are comparable to that of topotecan, one of topoisomerase I inhibitors. (c) 2008 Qi Dong You. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.