Design, synthesis and biological evaluation of substituted 11H-benzo[a]carbazole-5-carboxamides as novel antitumor agents

A series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were designed, synthesized and evaluated for their antitumor activity against human cancer A549 and HCT-116 cell lines. Most of the compounds showed potent antitumor activities, and compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.

Graphical abstractA series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were designed, synthesized and evaluated for their antitumor activity against human cancer A549 and HCT-116 cell lines. Compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were synthesized. ► Synthesized compounds were evaluated against human cancer A549 and HCT-116 cell lines. ► The most potent compound 8 can be prepared to the physiologically acceptable salt which improves the solubility greatly. ► Compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.