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N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors

✍ Scribed by Milan Bruncko; Stephen K. Tahir; Xiaohong Song; Jun Chen; Hong Ding; Jeffrey R. Huth; Sha Jin; Russell A. Judge; David J. Madar; Chang H. Park; Cheol-Min Park; Andrew M. Petros; Christin Tse; Saul H. Rosenberg; Steven W. Elmore

Book ID: 104004980
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 688 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.010

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✦ Synopsis

We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors (9) targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation.

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