期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 8, 页码 2410-2414出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.02.073
关键词
Akt kinase inhibitors
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. (C) 2011 Elsevier Ltd. All rights reserved.
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