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Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26.

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

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  • 1Array BioPharma Inc., 3200 Walnut Street, Boulder, CO 80301, USA. rxu@arraybiopharma.com

Abstract

We describe the design and synthesis of novel bicyclic spiro sulfonamides as potent Akt inhibitors. Through structure-based rational design, we have successfully improved PKA selectivity of previously disclosed spirochromanes. Representative compounds showed favorable Akt potency while exhibiting up to 1000-fold selectivity against PKA.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21420856
[PubMed - indexed for MEDLINE]
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