Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA
2011
Xu, Rui | Banka, Anna | Blake, James F. | Mitchell, Ian S. | Wallace, Eli M. | Bencsik, Josef R. | Kallan, Nicholas C. | Spencer, Keith L. | Gloor, Susan L. | Martinson, Matthew | Risom, Tyler | Gross, Stefan D. | Morales, Tony H. | Wu, Wenyi | Vigers, Guy P.A. | Brandhuber, Barbara J. | Skelton, Nicholas J.
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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