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Synthesis and Antitumor Activities of Novel Free Hydroxyl-containing Deguelin Derivatives |
HE Hai1,2, JIANG Zhi-hui2, ZHOU Xing-zi1,2, HE Sheng2, WU Xin-rong2 |
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Abstract Deguelin was prepared by three step reaction from Rotenone. Novel deguelin derivatives containing free hydroxyl groups(3a~3c and 4) were synthesized by boron tribromide demethylation or reduction with sodium cyanoborohydride from deguelin. The structures were characterized by 1H NMR, 13C NMR and LC-MS. The antitumor activities were investigated. The results showed that 12-hydroxyl deguelin(4) showed the best inhibition activities against MCF-7 and H1299 with IC50 of 0.11 μmol·L-1 and 0.01 μmol·L-1, respectively, which was better than deguelin.
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Received: 27 May 2015
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[1] |
. [J]. Chinese Journal of Synthetic Chemistry, 2015, 23(12): 0-0. |
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