Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.
نویسندگان
چکیده
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 IC(50)s against Lck in biochemical and cellular assays. These 4-amino-6-benzimidazole-pyrimidines represent a new class of tyrosine kinase inhibitors.
منابع مشابه
Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
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 poten...
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 18 20 شماره
صفحات -
تاریخ انتشار 2008