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

Research output: Contribution to journalArticle

41 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)2173-2176
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number8
DOIs
Publication statusPublished - 2006 Apr 15
Externally publishedYes

Fingerprint

Focal Adhesion Protein-Tyrosine Kinases
Chemical modification
Phosphotransferases
Pyrrolo(2,3-d)pyrimidine

Keywords

  • 7H-Pyrrolo[2,3-d]pyrimidines
  • Focal adhesion kinase
  • Inhibition
  • SAR

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. / Choi, Ha Soon; Wang, Zhicheng; Richmond, Wendy; He, Xiaohui; Yang, Kunyong; Jiang, Tao; Sim, Taebo; Karanewsky, Donald; Gu, Xiang Ju; Zhou, Vicki; Liu, Yi; Ohmori, Osamu; Caldwell, Jeremy; Gray, Nathanael; He, Yun.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 8, 15.04.2006, p. 2173-2176.

Research output: Contribution to journalArticle

Choi, HS, Wang, Z, Richmond, W, He, X, Yang, K, Jiang, T, Sim, T, Karanewsky, D, Gu, XJ, Zhou, V, Liu, Y, Ohmori, O, Caldwell, J, Gray, N & He, Y 2006, 'Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 8, pp. 2173-2176. https://doi.org/10.1016/j.bmcl.2006.01.053
Choi, Ha Soon ; Wang, Zhicheng ; Richmond, Wendy ; He, Xiaohui ; Yang, Kunyong ; Jiang, Tao ; Sim, Taebo ; Karanewsky, Donald ; Gu, Xiang Ju ; Zhou, Vicki ; Liu, Yi ; Ohmori, Osamu ; Caldwell, Jeremy ; Gray, Nathanael ; He, Yun. / Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. In: Bioorganic and Medicinal Chemistry Letters. 2006 ; Vol. 16, No. 8. pp. 2173-2176.
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