Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Jadhav, Vinod D.¹  Duerfeldt, Adam S.¹  Blagg, Brian S. J.¹ 

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

关键词: Hsp90;    Geldanamycin;    Radicicol;    Anti-cancer;   

DOI  :  10.1016/j.bmcl.2009.10.091

来源: Elsevier

【 摘 要 】

Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts. (C) 2009 Elsevier Ltd. All rights reserved.

【 授权许可】

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