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. 2010 Dec 15;20(24):7503-6.
doi: 10.1016/j.bmcl.2010.10.010. Epub 2010 Oct 12.

N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors

Milan Bruncko  1 , 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
Affiliations

N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors

Milan Bruncko et al. Bioorg Med Chem Lett. .

Abstract

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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