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Updated: Jun 6, 2026

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Malachite Green Assay for the Discovery of Heat-Shock Protein 90 Inhibitors
Published on: January 20, 2023
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors
Milan Bruncko1, Stephen K Tahir, Xiaohong Song
1Cancer Research, Global Pharmaceutical R&D, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. milan.bruncko@abbott.com
Bioorganic & Medicinal Chemistry Letters
|November 26, 2010
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.

