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

Choi, Ha-Soon and Wang, Zhicheng and Richmond, Wendy and He, Xiaohui and Yang, Kunyong and Jiang, Tao and Karanewsky, Donald and Gu, Xiang-Ju and Zhou, Vicki and Liu, Yi and Che, Jianwei and Lee, Christian and Caldwell, Jeremy and Kanazawa, Takanori and Umemura, Ichiro and Matsuura, Naoko and Ohmori, Osamu and Honda, Toshiyuki and 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
Related URLs:
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

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