Optimization of the Natural Product Calothrixin A to Discover Novel Dual Topoisomerase I and II Inhibitors with Improved Anticancer Activity

Optimization of the Natural Product Calothrixin A to Discover Novel Dual Topoisomerase I and II Inhibitors with Improved Anticancer Activity

Calothrixin A (CAA) is a dual Topo I and II inhibitor but exhibits poor antiproliferative activities and water solubility. Herein, a library of novel CAA analogues was synthesized. Among them, compound F16 exhibited superior water solubility (>5 mg/mL) as compared to CAA (

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Veröffentlicht in:Journal of medicinal chemistry 2022-06, Vol.65 (11), p.8040-8061
Hauptverfasser: Yang, Xiaohong, Wang, Zhi-Peng, Xiang, Sichuan, Wang, Daoqiang, Zhao, Yi, Luo, Dong, Qiu, Yanfei, Huang, Chao, Guo, Jian, Dai, Yuanwei, Zhang, Shao-Lin, He, Yun
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Sprache:eng
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Zusammenfassung:Calothrixin A (CAA) is a dual Topo I and II inhibitor but exhibits poor antiproliferative activities and water solubility. Herein, a library of novel CAA analogues was synthesized. Among them, compound F16 exhibited superior water solubility (>5 mg/mL) as compared to CAA (
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.2c00615