| Literature DB >> 16524731 |
Ha-Soon Choi1, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Jianwei Che, Christian C Lee, Jeremy Caldwell, Takanori Kanazawa, Ichiro Umemura, Naoko Matsuura, Osamu Ohmori, Toshiyuki Honda, Nathanael Gray, Yun He.
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 IC(50) and represents one of the most potent FAK inhibitors discovered to date.Entities:
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Year: 2006 PMID： 16524731 DOI： 10.1016/j.bmcl.2006.02.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823