N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
- Abbott
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.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
- Sponsoring Organization:
- INDUSTRY
- OSTI ID:
- 1025647
- Journal Information:
- Bioorg. Med. Chem. Lett., Vol. 20, Issue (24) ; 12, 2010
- Country of Publication:
- United States
- Language:
- ENGLISH
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