Title of article
Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors
Author/Authors
Jun Tang، نويسنده , , Toshihiro Hamajima، نويسنده , , Masato Nakano، نويسنده , , Hitoshi Sugawara and Hideyuki Sato، نويسنده , , Scott H. Dickerson، نويسنده , , Karen E. Lackey، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
4610
To page
4614
Abstract
The synthesis of a 7-azaindole series of novel, potent B-Raf kinase inhibitors using knowledge-based design was carried out. Compound 6h exhibits not only excellent potency in both the enzyme assay (IC50 = 2.5 nM) and the cellular assay (IC50 = 63 nM), but also has an outstanding selectivity profile against other kinases.
Keywords
7-Azaindole , Knowledge-based design , B-Raf kinase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799841
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