作为粘着斑激酶抑制剂的7H-吡咯并[2,3-d]嘧啶的设计与合成。第1部分。
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
作者信息
Choi Ha-Soon, Wang Zhicheng, Richmond Wendy, He Xiaohui, Yang Kunyong, Jiang Tao, Sim Taebo, Karanewsky Donald, Gu Xiang-ju, Zhou Vicki, Liu Yi, Ohmori Osamu, Caldwell Jeremy, Gray Nathanael, He Yun
机构信息
Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 920121, USA.
出版信息
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2173-6. doi: 10.1016/j.bmcl.2006.01.053. Epub 2006 Feb 3.
A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to target focal adhesion kinase (FAK). A number of these pyrrolopyrimides exhibited low micromolar inhibitory activities against focal adhesion kinase, and their preliminary SAR was established via systematic chemical modifications. The 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines represent a new class of kinase inhibitors.
设计并合成了一系列2-氨基-9-芳基-7H-吡咯并[2,3-d]嘧啶，以靶向粘着斑激酶（FAK）。其中许多吡咯并嘧啶对粘着斑激酶表现出低微摩尔抑制活性，并通过系统的化学修饰建立了它们的初步构效关系。2-氨基-9-芳基-7H-吡咯并[2,3-d]嘧啶代表了一类新型的激酶抑制剂。
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