|
|||||
|
|
Discovery and SAR of spirochromane Akt inhibitors |
|
| Authors: | 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 |
| Institution: | a Array BioPharma, Inc., 3200 Walnut Street, Boulder, CO 80301, USA b Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080-4990, USA |
| Abstract: | 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. |
| Keywords: | Akt kinase inhibitors |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |