N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors

Bioorganic & Medicinal Chemistry Letters
2010.0

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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