CAS: 1157857-29-8; 3-Nitro-4-Methyl-N-(3-(4-Methyl-1H-Imidazol-1-yl)-5(Trifluoromethyl)Phenyl)Benzamide

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3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)aniline 4-methyl-3-nitrobenzoyl chloride 4-methyl-3-nitrobenzoic acid 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-aminobenzamide

📜4-甲基-3-硝基苯甲酸置于氯化亚砜,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应生成3-硝基-4-甲基-N-(3-(4-甲基-1H-咪唑-1-基)-5-(三氟甲基)苯基)苯甲酰胺
参考文献:Design,Synthesis And Biological Evaluation Of Novel Acrylamide Analogues As Inhibitors Of Bcr-abl Kinase
标题:Design,Synthesis And Biological Evaluation Of Novel Acrylamide Analogues As Inhibitors Of Bcr-abl Kinase
摘要:A Series Of Acrylamide Analogues Were Designed And Synthesized From Imatinib And Nilotinib As Novel Bcr-Abl Inhibitors By Application Of The Principle Of Nonclassical Electronic Isostere. All New Compounds Were Evaluated For Their Inhibitory Effects On The Activity Of Bcr-Abl Kinase And The Proliferation Of K562 Leukemia Cancer Cells In Vitro. The Acrylamide Analogues In Which The Substituent In C Ring Was Trifluoromethyl Group Were Identified As Highly Potent Bcr-Abl Kinase Inhibitors. Compound 13F Exhibited An Ic50 Value As Low As 20.6 Nm In Abl Kinase Inhibition And An Ic50 Value Of 32.3 Nm For Antiproliferative Activity,About 10.5-Fold And 12-Fold Lower Than Those Of Imatinib Respectively. These Results Suggest That Compound 13F Is A Promising Candidate As A Novel Bcr-Abl Kinase Inhibitor For Further Development. (C) 2012 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2012.06.044