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- Park, Cheol-Min
- Synthetic and Medicinal Chemistry Lab.
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N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
- Author(s)
- 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.
- Issued Date
- 2010-12
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.24, pp.7503 - 7506
- 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.
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- ISSN
- 0960-894X
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