Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371149 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rui Xu, Anna Banka, James F. Blake, Ian S. Mitchell, Eli M. Wallace, Josef R. Bencsik, Nicholas C. Kallan, Keith L. Spencer, Susan L. Gloor, Matthew Martinson, Tyler Risom, Stefan D. Gross, Tony H. Morales, Wen-I Wu, Guy P.A. Vigers,