1307262-65-2Relevant articles and documents
Discovery and SAR of spirochromane Akt inhibitors
Kallan, Nicholas C.,Spencer, Keith L.,Blake, James F.,Xu, Rui,Heizer, Justin,Bencsik, Josef R.,Mitchell, Ian S.,Gloor, Susan L.,Martinson, Matthew,Risom, Tyler,Gross, Stefan D.,Morales, Tony H.,Wu, Wen-I,Vigers, Guy P.A.,Brandhuber, Barbara J.,Skelton, Nicholas J.
scheme or table, p. 2410 - 2414 (2011/05/15)
A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA.
