Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 20, Pages 6495-6502Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm8007486
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Funding
- University of Kansas
- American Foundation for Pharmaceutical Education
- Madison and Lila Self Graduate Fellowship Program
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Gedunin (1), a tetranortriterpenoid isolated from the Indian neern tree (Azadirachta indica), was recently shown to manifest anticancer activity via inhibition of the 90 kDa heat shock protein (Hsp90) folding machinery and to induce the degradation of Hsp90-dependent client proteins similar to other Hsp90 inhibitors. The mechanism of action by which gedunin induces client protein degradation remains undetermined, however, prior studies have demonstrated that it does not bind competitively versus ATP. In an effort to further probe the mechanism of action, 19 semisynthetic derivatives of gedunin were prepared and their antiproliferative activity against MCF-7 and SkBr3 breast cancer cells determined. Although no compound was found to exhibit antiproliferative activity more effective than the natural product, functionalities critical for antiproliferative activity have been identified.
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