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Design and Synthesis of 1‐(6‐(2‐(2‐Arylethynyl)Phenyl)Hexyn‐5‐yl)Piperidin‐2‐Ones as Antitumor Agents that Induce Apoptotic Progress
Author(s) -
Lin ILing,
Chen IHsiang,
Lin ChiFong,
Lo YuHsiang,
Yang ShengHuei,
Lin ShinneRen,
Wu MingJung
Publication year - 2008
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.200800100
Subject(s) - chemistry , apoptosis , potency , cell culture , stereochemistry , leukemia , cell cycle , combinatorial chemistry , in vitro , biochemistry , medicine , genetics , biology
Abstract A series of 1‐(6‐(2‐(2‐arylethynyl)phenyl)hexyn‐5‐yl)piperidin‐2‐ones 2a‐j were synthesized and their antitumor activities were evaluated. Of these compounds, 1‐(6‐(2‐(2‐(4‐nitrophenyl)ethynyl)phenyl)hexyn‐5‐yl)piperidin‐2‐one ( 2j ) showed the highest potency of growth inhibition activity, especially against the RPMI‐8226 (0.4 μM) and SR (0.02 μM) cell lines of human leukemia. Compound 2j also induced significant apoptotic progress in the cell cycle assay with the K‐562 cell line.