Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors

The design, synthesis and biological evaluation of novel triazolyl p38α MAPK inhibitors with improved water solubility for formulation in cationic liposomes (SAINT-O-Somes) targeted at diseased endothelial cells is described. Water-solubilizing groups were introduced via a 'click' reaction...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-03, Vol.24 (5), p.1352-1357
Hauptverfasser:	Seerden, Jean-Paul G, Leusink-Ionescu, Gabriela, Leguijt, Robin, Saccavini, Catherine, Gelens, Edith, Dros, Bas, Woudenberg-Vrenken, Titia, Molema, Grietje, Kamps, Jan A A M, Kellogg, Richard M
Format:	Artikel
Sprache:	eng
Schlagworte:	Human Umbilical Vein Endothelial Cells Humans Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - metabolism Liposomes - chemistry p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors p38 Mitogen-Activated Protein Kinases - metabolism Protein Binding Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Solubility Structure-Activity Relationship Triazoles - chemical synthesis Triazoles - chemistry Triazoles - metabolism Water - chemistry
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