N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
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- N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
- Bruncko, Milan; Tahir, Stephen K.; Song, Xiaohong; Chen, Jun; Ding, Hong; Huth, Jeffrey R.; Jin, Sha; Judge, Russell A.; Madar, David J.; Park, Chang H.; Park, Cheol-Min; Petros, Andrew M.; Tse, Christin; Rosenberg, Saul H.; Elmore, Steven W.
- Issue Date
- PERGAMON-ELSEVIER SCIENCE LTD
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.24, pp.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.
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