National Center for
3OW6: Crystal Structure Of Hsp90 With N-Aryl-Benzimidazolone I
Bioorg. Med. Chem. Lett. (2010) 20 p.7503-7506
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.