Design, synthesis, and evaluation of a radicicol and geldanamycin chimera, radamide

被引：62
作者：
Clevenger, RC
Blagg, BSJ
机构：
[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA
[2] Univ Kansas, Ctr Prot Struct & Funct, Lawrence, KS 66045 USA
来源：
ORGANIC LETTERS | 2004年 / 6卷 / 24期
关键词：
D O I：
10.1021/ol048266o
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A chimera composed of the natural products radicicol and geldanamycin has been prepared through an amide linkage connecting the resorcinol moiety of radicicol to the quinone ring of geldanamycin. The inhibitory activity of these compounds was determined by their ability to inhibit Hsp90's inherent ATPase activity along with degradation of the Hsp90 client protein, HER-2 in MCF-7 breast cancer cells.
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收藏
页码：4459 / 4462
页数：4
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