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The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors

Authors :
Tang, Jun
Lackey, Karen E.
Dickerson, Scott H.
Source :
Bioorganic & Medicinal Chemistry Letters. Jan2013, Vol. 23 Issue 1, p66-70. 5p.
Publication Year :
2013

Abstract

Abstract: A series of novel, potent 4-aminothienopyridine B-Raf kinase inhibitors was designed and synthesized using knowledge-based design. Compounds 5f, and 6k exhibited not only excellent potency in both enzyme assay (IC50 =5.1, 16.6nM) and cellular assay (IC50 =0.2, 0.2μM), but also had an outstanding selectivity profile against other kinases. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
23
Issue :
1
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
84360553
Full Text :
https://doi.org/10.1016/j.bmcl.2012.11.020