Design and synthesis of 7H-pyrrolo [2, 3-d] pyrimidines as focal adhesion kinase inhibitors. Part 2

…, CC Lee, J Caldwell, T Kanazawa, I Umemura…

Index: Choi, Ha-Soon; Wang, Zhicheng; Richmond, Wendy; He, Xiaohui; Yang, Kunyong; Jiang, Tao; Karanewsky, Donald; Gu, Xiang-ju; Zhou, Vicki; Liu, Yi; Che, Jianwei; Lee, Christian C.; Caldwell, Jeremy; Kanazawa, Takanori; Umemura, Ichiro; Matsuura, Naoko; Ohmori, Osamu; Honda, Toshiyuki; Gray, Nathanael; He, Yun Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2689 - 2692

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Citation Number: 59

Abstract

A series of 2-amino-9-aryl-7H-pyrrolo [2, 3-d] pyrimidines were designed and synthesized as focal adhesion kinase (FAK) inhibitors using molecular modeling in conjunction with a co- crystal structure. Chemistry was developed to introduce functionality onto the 9-aryl ring, which resulted in the identification of potent FAK inhibitors. In particular, compound 32 possessed single-digit nanomolar IC50 and represents one of the most potent FAK ...