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Synthesis, cytotoxicity and apoptosis‐inducing activity of novel 1 H ‐benzo[ d ]imidazole derivatives of dehydroabietic acid
Author(s) -
Li ALiang,
Yang YaQun,
Wang WenYan,
Liu QingSong,
Sun Yue,
Gu Wen
Publication year - 2020
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.202000075
Subject(s) - chemistry , hela , apoptosis , cytotoxicity , cell culture , cytotoxic t cell , benzamide , cancer cell , imidazole , cell cycle checkpoint , cell cycle , stereochemistry , cell , biochemistry , cancer , in vitro , biology , genetics
With the expectation of finding new and effective antitumor drugs, a series of novel N ‐(1 H ‐benzo[ d ]imidazole‐2‐yl)‐benzamide/benzenesulfonamide derivatives of dehydroabietic acid were synthesized and evaluated for cytotoxic activity against three human cancer cell lines (MCF‐7, HeLa, and HepG2 cells) and one human normal hepatocyte cell line (LO2). As a result, a number of derivatives showed moderate to good antitumor activities. Among them, compound 8h exhibited the most potent activities against three cancer cell lines with IC 50 values of 0.87 ± 0.18, 9.39 ± 0.72, and 8.31 ± 0.64 μM, respectively, and was less active to normal hepatocyte LO2 cells. Further mechanism studies revealed that compound 8h could arrest the cell cycle of MCF‐7 cells at S phase and induce the apoptosis of MCF‐7 cells in ROS‐mediated mitochondrial pathway.