Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I

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

Research output: Contribution to journalArticle

32 Citations (Scopus)


A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src kinase family. Highly efficient parallel syntheses were devised to prepare analogues for SAR studies. A number of these 4-amino-6-benzimidazole-pyrimidines exhibited single-digit nanomolar IC50s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.

Original languageEnglish
Pages (from-to)5618-5621
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Publication statusPublished - 2008 Oct 15
Externally publishedYes


  • 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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    Zhang, G., Ren, P., Gray, N. S., Sim, T., Liu, Y., Wang, X., Che, J., Tian, S. S., Sandberg, M. L., Spalding, T. A., Romeo, R., Iskandar, M., Chow, D., Martin Seidel, H., Karanewsky, D. S., & He, Y. (2008). Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I. Bioorganic and Medicinal Chemistry Letters, 18(20), 5618-5621.