发现和 SAR 研究螺环 chromane Akt 抑制剂。
Discovery and SAR of spirochromane Akt inhibitors.
机构信息
Array BioPharma, Inc., 3200 Walnut Street, Boulder, CO 80301, USA.
出版信息
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18.
PMID:21392984
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.
摘要
报告了一系列新型的螺环色满 pan-Akt 抑制剂。SAR 优化提供了具有改善的酶活性和对相关 AGC 激酶 PKA 优异选择性的化合物。尝试用酚羟基铰链配体替代提供了具有优异 Akt 酶和细胞活性但对 PKA 选择性大大降低的化合物。
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