Design, Synthesis, and Biological Evaluation of Conformationally Constrained cis-Amide Hsp90 Inhibitors

被引：24

作者：

Duerfeldt, Adam S. ^{[1
]}

Brandt, Gary E. L. ^{[1
]}

Blagg, Brian S. J. ^{[1
]}

机构：

[1] Univ Kansas, Dept Med Chem, Lawrence, KS 66045 USA

来源：

ORGANIC LETTERS | 2009年 / 11卷 / 11期

关键词：

MOLECULAR CHAPERONES; CHIMERIC INHIBITORS; TUMOR SELECTIVITY; BINDING-SITE; GELDANAMYCIN; PROTEIN; RADICICOL; TARGET; CANCER; EXPLANATION;

D O I：

10.1021/ol900783m

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Conformationally constrained cis-amide chimeric inhibitors of Hsp90 have been synthesized and evaluated for their Hsp90 inhibitory activity. These new compounds exhibited Hsp90 ATPase inhibition and induced Hsp90-dependent client protein degradation in a dose-dependent manner. Biological data reported herein suggests that amide bond isomerization of geldanamycin derivatives plays an important role in affinity for the heteroprotein complex present in cancer cells.

引用

页码：2353 / 2356

页数：4

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