Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1

Ha-Soon Choi; Zhicheng Wang; Wendy Richmond; Xiaohui He; Kunyong Yang; Tao Jiang; Taebo Sim; Donald Karanewsky; Xiang-ju Gu; Vicki Zhou; Yi Liu; Osamu Ohmori; Jeremy Caldwell; Nathanael Gray; Yun He

doi:10.1016/j.bmcl.2006.01.053

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2173-6. doi: 10.1016/j.bmcl.2006.01.053. Epub 2006 Feb 3.

Authors

Ha-Soon Choi¹, Zhicheng Wang, Wendy Richmond, Xiaohui He, Kunyong Yang, Tao Jiang, Taebo Sim, Donald Karanewsky, Xiang-ju Gu, Vicki Zhou, Yi Liu, Osamu Ohmori, Jeremy Caldwell, Nathanael Gray, Yun He

Affiliation

¹ Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 920121, USA.

PMID: 16458503
DOI: 10.1016/j.bmcl.2006.01.053

Abstract

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.

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Cell Line, Tumor
Drug Screening Assays, Antitumor
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Focal Adhesion Protein-Tyrosine Kinases / antagonists & inhibitors*
Humans
Pyrimidines / chemical synthesis
Pyrimidines / pharmacology
Pyrroles / chemical synthesis
Pyrroles / pharmacology
Structure-Activity Relationship

Substances

Antineoplastic Agents
Enzyme Inhibitors
Pyrimidines
Pyrroles
Focal Adhesion Protein-Tyrosine Kinases