Akt1 和 Akt2 的变构抑制剂：具有强效和平衡活性的[1,2,4]三唑并[3,4-f][1,6]萘啶的发现。
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., 770 Sumneytown Pike, WP14-2, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2009 Feb 1;19(3):834-6. doi: 10.1016/j.bmcl.2008.12.017. Epub 2008 Dec 7.
PMID:19097777
Abstract
A series of [1,2,4]triazolo[3,4-f][1,6]naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory activity against Akt1 and 2 in vivo in a mouse model.
摘要
已经开发出一系列[1,2,4]三唑并[3,4-f][1,6]萘啶类 Akt1 和 2 的别构双抑制剂。这些化合物表现出对 Akt1 和 2 的双重细胞效力。代表性化合物 13 在小鼠模型中表现出对 Akt1 和 2 的体内强烈抑制活性。
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