Synthesis of rotenoid derivatives with cytotoxic and topoisomerase II inhibitory activities

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• 作者：Supranee Sangthong^a ; Kuakarun Krusong^b ; Nattaya Ngamrojanavanich^c ; Tirayut Vilaivan^c ; Songchan Puthong^d ; Supajittra Chandchawan^e ; Nongnuj Muangsin^c ; ^{nongnuj.j@chula.ac.th"" rel=""nofollow}
• 关键词：Rotenoids ; DNA-binding ; Topoisomerase II inhibition ; Anticancer activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 August 2011
• 年：2011
• 卷：21
• 期：16
• 页码：4813-4818
• 全文大小：510 K

文摘

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 IC₅₀ 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.