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Synthesis of rotenoid derivatives with cytotoxic and topoisomerase II inhibitory activities. 2011
Supranee Sangthong, and
Kuakarun Krusong, and
Nattaya Ngamrojanavanich, and
Tirayut Vilaivan, and
Songchan Puthong, and
Supajittra Chandchawan, and
Nongnuj Muangsin
Program of Biotechnology, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Bangkok 10330, Thailand.
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.
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