发现2,3,5-三取代吡啶衍生物作为有效的Akt1和Akt2双重抑制剂。
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
作者信息
Zhao Zhijian, Leister William H, Robinson Ronald G, Barnett Stanley F, Defeo-Jones Deborah, Jones Raymond E, Hartman George D, Huff Joel R, Huber Hans E, Duggan Mark E, Lindsley Craig W
机构信息
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck Research Laboratories, Merck & Co., PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2005 Feb 15;15(4):905-9. doi: 10.1016/j.bmcl.2004.12.062.
This letter describes the discovery of a novel series of dual Akt1/Akt2 kinase inhibitors, based on a 2,3,5-trisubstituted pyridine scaffold. Compounds from this series, which contain a 5-tetrazolyl moiety, exhibit more potent inhibition of Akt2 than Akt1.
这封信描述了基于2,3,5-三取代吡啶支架发现的一系列新型Akt1/Akt2双激酶抑制剂。该系列化合物含有一个5-四唑基部分，对Akt2的抑制作用比对Akt1更强。
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