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

…, B Dros, T Woudenberg-Vrenken, G Molema…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 5 p. 1352 - 1357

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被引用次数: 7

摘要

Abstract 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 of functional azides with 2-alkynyl imidazoles and isosteric oxazoles to generate two small libraries of 1, 4-disubstituted 1, 2, 3-triazolyl p38α MAPK ...