2. Academic Validation
  3. Synthesis of rotenoid derivatives with cytotoxic and topoisomerase II inhibitory activities

Synthesis of rotenoid derivatives with cytotoxic and topoisomerase II inhibitory activities

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4813-8. doi: 10.1016/j.bmcl.2011.06.052.
Supranee Sangthong 1,  Kuakarun Krusong,  Nattaya Ngamrojanavanich,  Tirayut Vilaivan,  Songchan Puthong,  Supajittra Chandchawan,  Nongnuj Muangsin
Affiliations

Affiliation

  • 1 Program of Biotechnology, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Bangkok 10330, Thailand.
PMID: 21741833 DOI: 10.1016/j.bmcl.2011.06.052
Abstract

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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