Calothrixin A () is a dual Topo I and II inhibitor but exhibits poor antiproliferative activities and water solubility. Herein, a library of novel analogues was synthesized. Among them, compound exhibited superior water solubility (>5 mg/mL) as compared to (<5 μg/mL). The mechanism of action studies confirmed that acted as a dual Topo I and II poison. Furthermore, displayed potent antiproliferative activities against high Topo I and II expression cell lines A375 and HCT116, with IC values of 20 and 50 nM, respectively. In xenograft models, reduced the tumor growth at a dose of 10 or 20 mg/kg without apparent effect on the mouse weight, while the clinically used Topo II inhibitor dramatically reduced the mouse weight. Collectively, our data demonstrated that could be a promising lead for the development of novel dual Topo I and II antitumor agents.
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