Program of Biotechnology, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Bangkok 10330, Thailand.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4813-8. doi: 10.1016/j.bmcl.2011.06.052. Epub 2011 Jul 7.
6-Deoxyclitoriacetal (1) and a series of 11 further derivatives of it (2-12) were synthesized and evaluated for their cytotoxic and topoisomerase IIα inhibitory activities. Compounds bearing epoxide (2), morpholine (6) and benzylamine (10) moieties showed promising in vitro cytotoxic activities against four cancer cell lines, with IC(50) values ranging from 0.38 to 0.73 μM. These three compounds also strongly inhibited topoisomerase II activity at 68.3-93.5% and showed a moderately high DNA intercalating property.
6-去氧环他定（1）及其一系列 11 种进一步的衍生物（2-12）被合成并评估了其细胞毒性和拓扑异构酶 IIα抑制活性。带有环氧化物（2）、吗啉（6）和苄胺（10）部分的化合物对四种癌细胞系表现出有希望的体外细胞毒性活性，IC50 值范围为 0.38 至 0.73 μM。这三种化合物还强烈抑制拓扑异构酶 II 活性，抑制率为 68.3-93.5%，并显示出适度高的 DNA 插入性质。
