Telescoped Synthesis of 2-Acyl-1-aryl-1,2-dihydroisoquinolines and Their Inhibition of the Transcription Factor NF-魏B

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• 作者：Tsai-Wen Chung ; Yi-Tzu Hung ; Tushar Thikekar ; Vijaykumar V. Paike ; Fu Yuan Lo ; Pei-Hua Tsai ; Mei-Chih Liang ; Chung-Ming Sun
• 刊名：ACS Combinatorial Science
• 出版年：2015
• 出版时间：August 10, 2015
• 年：2015
• 卷：17
• 期：8
• 页码：442-451
• 全文大小：680K
• ISSN：2156-8944

文摘

A sequential single-flask multicomponent reactions is highly effective for the synthesis of 1,2-dihydroisoquinolines through amidealkylation from intermediate N-acylisoquinolinium salts under mild conditions. N-Acylisoquinolinium ions and trichloromethyl-1-(1H-indol-3-yl)isoquinoline-2(1H)-carboxylate have demonstrated their reactivity toward aromatic and aliphatic 蟺-nucleophiles. One of the 1,2-dihydroisoquinoline derivatives was found to be a potent inhibitor for transcription factor NF-魏B by blocking I魏B伪 degradation, p65 nuclear translocation, and NF-魏B DNA binding in TNF-伪-induced NIH 3T3 cells.