期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 13, 页码 3957-3960出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.140
关键词
Hsp90; Novobiocin; Antiproliferation; Triazole
资金
- NIH [CA120458, T32 GM008545]
A series of triazole-containing novobiocin analogues has been designed, synthesized and their inhibitory activity determined. These compounds contain a triazole ring in lieu of the amide moiety present in the natural product. The anti-proliferative effects of these compounds were evaluated against two breast cancer cell lines ( SKBr-3 and MCF-7), and manifested activities similar to their amide-containing counterparts. In addition, Hsp90-dependent client protein degradation was observed via Western blot analyses, supporting a common mode of Hsp90 inhibition for both structural classes. (C) 2010 Elsevier Ltd. All rights reserved.
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