Synthesis and MEK1 inhibitory activities of imido-Substituted 2-chloro-1,4-naphthoquinones

Mitogen activated protein kinases are of interest as research tools and as therapeutic target for certain physiological disorders. In this study, we found 2-chloro-3-( N-succinimidyl)-1,4-naphthoquinone 6 to be a selective inhibitor of MEK1 with an IC 50 of 0.38 μM. An open-chain homologue, 10, show...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2003-07, Vol.11 (14), p.3165-3170
Hauptverfasser:	Bakare, Oladapo, Ashendel, Curtis L., Peng, Hairuo, Zalkow, Leon H., Burgess, Edward M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Biological and medical sciences Cell Line, Tumor Cyclic AMP - metabolism Cyclic AMP-Dependent Protein Kinases - antagonists & inhibitors Drug Design Drug Screening Assays, Antitumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology General aspects Humans Imides - chemistry MAP Kinase Kinase 1 Medical sciences Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors Molecular Structure Naphthoquinones - chemical synthesis Naphthoquinones - pharmacology Pharmacology. Drug treatments Protein Kinase C - antagonists & inhibitors Structure-Activity Relationship
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