Browsing by Author "Thikekar, Tushar"

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Telescoped Synthesis of 2-Acyl-1-aryl-1,2-dihydroisoquinolines and Their Inhibition of the Transcription Factor NF-kappa B
(2015-08-01)
Chung, Tsai-Wen
;
Hung, Yi-Tzu
;
Thikekar, Tushar
;
Paike, Vijaykumar V.
;
Lo, Fu Yuan
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 pi-nucleophiles. One of the 1,2-dihydroisoquinoline derivatives was found to be a potent inhibitor for transcription factor NF-kappa B by blocking I kappa B alpha degradation, p65 nuclear translocation, and NF-kappa B DNA binding in TNF-alpha-induced NIH 3T3 cells.