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[摘要]：Three series of novel spin-labeled rotenone derivatives were synthesized and evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB and KBvin. All of the derivatives showed promising in vitro cytotoxic activity against the tumor cell lines tested, with IC50 values ranging from 0.075 to 0.738 mu g/mL. Remarkably, all of the compounds were more potent than paclitaxel against KBvin in vitro, and compounds 3a and 3d displayed the highest cytotoxicity against this cell line (IC50 0.075 and 0.092 mu g/mL, respectively). Based on the observed cytotoxicity, structure-activity relationships have been described. (C) 2011 Elsevier Ltd. All rights reserved. |
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