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

Abstract:

: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 π-nucleophiles. One of the 1,2-dihydroisoquinoline derivatives was found to be a potent inhibitor for transcription factor NF-κB by blocking IκBα degradation, p65 nuclear translocation, and NF-κB DNA binding in TNF-α-induced NIH 3T3 cells.

journal_name

ACS Comb Sci

authors

Chung TW,Hung YT,Thikekar T,Paike VV,Lo FY,Tsai PH,Liang MC,Sun CM

doi

10.1021/acscombsci.5b00001

subject

Has Abstract

pub_date

2015-08-10 00:00:00

pages

442-51

issue

8

eissn

2156-8952

issn

2156-8944

journal_volume

17

pub_type

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