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Synthesis and Antiproliferative Evaluation of 4‐Anilino‐ n ‐methoxyfuro[2,3‐ b ]quinoline Derivatives ( n =6, 7). Part 5
Author(s) -
Chen YehLong,
Lin HuanChin,
Yang ChiaNing,
Lu PeiJung,
Tzeng CherngChyi
Publication year - 2008
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200890024
Subject(s) - hela , chemistry , quinoline , cell cycle , flow cytometry , cell cycle progression , cell growth , cell cycle checkpoint , fragmentation (computing) , dna fragmentation , stereochemistry , a549 cell , cell culture , dna , cell , microbiology and biotechnology , apoptosis , programmed cell death , biochemistry , biology , organic chemistry , genetics , ecology
A series of 27 differently substituted 4‐anilinofuro[2,3‐ b ]quinolines were synthesized and evaluated for their antiproliferative activities against the HeLa, SKHep1, SAS, AGS, A549, and CE81T cell lines, cancers commonly found in Asian countries. Among the compounds tested, 1‐{4‐[(3‐chloro‐7‐methoxyfuro[2,3‐ b ]quinolin‐4‐yl)amino]phenyl}ethanone ( 1 ) was the most potent, with IC 5 0 values of 3.1, 3.0, and 4.2 μ M , resp., against the growth of HeLa, SKHep, and CE81T cells. Compound 1 was, thus, further evaluated by flow cytometry to evaluate its effect on the cell‐cycle distribution of HeLa cells. Our results indicated that 1 readily induces cell‐cycle arrest in the G2/M phase, followed by DNA fragmentation and, ultimately, cell death.