Title of article
Discovery of pyrimidine benzimidazoles as Lck inhibitors: Part I
Author/Authors
Guobao Zhang، نويسنده , , Pingda Ren، نويسنده , , Nathanael S. Gray، نويسنده , , Taebo Sim، نويسنده , , Yi Liu، نويسنده , , Xia Wang، نويسنده , , Jianwei Che، نويسنده , , Shin-Shay Tian، نويسنده , , Mark L. Sandberg، نويسنده , , Tracy A. Spalding، نويسنده , , Russell Romeo، نويسنده , , Maya Iskandar، نويسنده , , Donald Chow، نويسنده , , H. Martin Seidel، نويسنده , , Donald S. Karanewsky، نويسنده , , Yun He، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
5618
To page
5621
Abstract
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.
Keywords
Lck inhibitor , kinase inhibitor , Transplantation rejection , autoimmune disease , Pyrimidine benzimidazoles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800071
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