📜3-硝基苯乙酸置于palladium On Activated Charcoal Ammonium Hydroxide,氢气,三乙胺体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,25.0~140.0 °C,101.33 Kpa 条件下,反应 37.0H,反应生成3-(3-氨基苯基)-4-(1-甲基-1H-吲哚-3-基)吡咯-2,5-二酮
参考文献:Inhibitors Of Protein Kinase C. 1. 2,3-Bisarylmaleimides
标题:Inhibitors Of Protein Kinase C. 1. 2,3-Bisarylmaleimides
摘要:The Design And Synthesis Of A Series Of Novel Inhibitors Of Protein Kinase C (Pkc) Is Described. These 2,3-Bisarylznaleimides Were Derived From The Structural Lead Provided By The Indolocarbazoles,Staurosporine And K252A. Optimum Activity Required The Imide Nh,Both Carbonyl Groups,And The Olefinic Bond Of The Maleimide Ring. 2,3-Bisindolylmaleimides Were The Most Active,And The Potency Of These Was Improved By A Chloro Substituent At The 5-Position Of One Indole Ring (Compound 28,Ic50 0.11-Mu-M). In A Series Of (Phenylindolyl)Maleimides,Nitro Compound 74 Was Most Active (Ic50 0.67-Mu-M). Naphthalene 19 And Benzothiophene 21 Showed Greater Than 100-Fold Selectivity For Inhibition Of Pkc Over The Closely Related Camp-Dependent Protein Kinase (Pka).
Doi:10.1021/jm00079A024