Ontology highlight
ABSTRACT:
SUBMITTER: Li J
PROVIDER: S-EPMC2789032 | biostudies-literature | 2009 Nov
REPOSITORIES: biostudies-literature
Li Jing J Kaoud Tamer S TS Laroche Christophe C Dalby Kevin N KN Kerwin Sean M SM
Bioorganic & medicinal chemistry letters 20090927 22
Based on the mild, thermal rearrangement of 1,2-dialkynylimidazoles to reactive carbene or diradical intermediates, a series of 1,2-dialkynylimidazoles were designed as potential irreversible p38 MAP kinase alpha-isoform (p38alpha) inhibitors. The synthesis of these dialkynylimidazoles and their kinase inhibition activity is reported. The 1-ethynyl-substituted dialkynylimidazole 14 is a potent (IC(50)=200 nM) and selective inhibitor of p38alpha. Moreover, compound 14 covalently modifies p38alpha ...[more]