Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors
The MAPK pathway is identified as one of the most important pathways involved in cell proliferation and differentiation. A key kinase in the pathway, the Mitogen-activated protein kinase kinase (MEK) is recognized as a promising target for antitumor drugs. Structure-based design and optimization of known MEK inhibitors resulted in identification of compound 10a as a potent non-ATP competitive MEK inhibitor in both in vitro and in vivo tests.
A facile synthesis of 5-halopyrimidine-4-carboxylic acid esters via a Minisci reaction
This paper reports the synthesis of various 5-halopyrimidine-4-carboxylic acid esters via the Minisci homolytic alkoxycarbonylation of 5-halopyrimidines. The reaction was found to be highly regioselective, allowing the one-step synthesis of useful amounts
Regan, Collin F.,Pierre, Fabrice,Schwaebe, Michael K.,Haddach, Mustapha,Jung, Michael E.,Ryckman, David M.
experimental part
p. 443 - 447
(2012/03/11)
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