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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
