Natural product-based design, synthesis and biological evaluation of anthra[2,1-d]thiazole-6,11-dione derivatives from rhein as novel antitumour agents

•Two series of novel rhein analogues were designed, synthesized and evaluated.•Screening the target products against cells A549 and HeLa in vitro was carried out.•Two out of the target compounds showed more potent activity than rhein.

Two series of novel 2-substituted 5,7-dihydroxyanthra[2,1-d]thiazole-6,11-dione derivatives from natural rhein were designed, synthesized and evaluated for their antitumour activities against human cancer cell lines A549 and HeLa in vitro.

Graphical abstractTwo series of novel 2-substituted 5,7-dihydroxyanthra[2,1-d]thiazole-6,11-dione derivatives from natural rhein were designed, synthesized and evaluated for their antitumour activities against human cancer cell lines A549 and HeLa in vitro.Figure optionsDownload full-size imageDownload as PowerPoint slide