Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II

Guobao Zhang, Pingda Ren, Nathanael S. Gray, Taebo Sim, Xia Wang, Yi Liu, Jianwei Che, Weitong Dong, Shin Shay Tian, Mark L. Sandberg, Tracy A. Spalding, Russell Romeo, Maya Iskandar, Zhiliang Wang, H. Martin Seidel, Donald S. Karanewsky, Yun He

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src-family kinases (SFKs). These type II inhibitors were optimized using a cellular Lck-dependent proliferation assay and are capable of inhibiting Lck at single-digit nanomolar concentrations. This scaffold is likely to serve a valuable template for developing potent inhibitors of a number of SFKs.

Original languageEnglish
Pages (from-to)6691-6695
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
Publication statusPublished - 2009 Dec 1
Externally publishedYes

Keywords

  • Autoimmune disease
  • Kinase inhibitor
  • Lck inhibitor
  • Pyrimidine benzimidazoles
  • Transplantation rejection

ASJC Scopus subject areas

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

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  • Cite this

    Zhang, G., Ren, P., Gray, N. S., Sim, T., Wang, X., Liu, Y., Che, J., Dong, W., Tian, S. S., Sandberg, M. L., Spalding, T. A., Romeo, R., Iskandar, M., Wang, Z., Seidel, H. M., Karanewsky, D. S., & He, Y. (2009). Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorganic and Medicinal Chemistry Letters, 19(23), 6691-6695. https://doi.org/10.1016/j.bmcl.2009.09.123