Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
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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, Caldwell, Jeremy, Kanazawa, Takanori, Umemura, Ichiro, Matsuura, Naoko, Ohmori, Osamu, Honda, Toshiyuki, Gray, Nathanael and He, Yun (2006) Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorganic & Medicinal Chemistry Letters, 16 (10). pp. 2689-2692. ISSN 0960-894X
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.
| Item Type: | Article |
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| Additional Information: | author can archive post-print (ie final draft post-refereeing) |
| Keywords: | 7H-Pyrrolo[2,3-d]pyrimidines; Focal adhesion kinase (FAK); Molecular modeling; SAR; Kinase inhibitor |
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| Date Deposited: | 14 Dec 2009 14:04 |
| Last Modified: | 31 Jan 2013 01:26 |
| URI: | https://oak.novartis.com/id/eprint/155 |