1. Synthesis and in vitro cytotoxic evaluation of new 1H-benzo[d]imidazole derivatives of dehydroabietic acid.
- Author
-
Gu W, Miao TT, Hua DW, Jin XY, Tao XB, Huang CB, and Wang SF
- Subjects
- Antineoplastic Agents toxicity, Cell Line, Cell Line, Tumor, Cell Survival drug effects, Hep G2 Cells, Humans, Imidazoles chemistry, Inhibitory Concentration 50, Molecular Structure, Abietanes chemistry, Antineoplastic Agents chemical synthesis, Imidazoles chemical synthesis, Imidazoles toxicity
- Abstract
A series of new 1H-benzo[d]imidazole derivatives of dehydroabietic acid were designed and synthesized as potent antitumor agents. Structures of the target molecules were characterized using MS, IR,
1 H NMR,13 C NMR and elemental analyses. In the in vitro cytotoxic assay, most compounds showed significant cytotoxic activities against two hepatocarcinoma cells (SMMC-7721 and HepG2) and reduced cytotoxicity against noncancerous human hepatocyte (LO2). Among them, compound 7b exhibited the best cytotoxicity against SMMC-7721 cells (IC50 : 0.36±0.13μM), while 7e was most potent to HepG2 cells (IC50 : 0.12±0.03μM). The cell cycle analysis indicated that compound 7b caused cell cycle arrest of SMMC-7721 cells at G2/M phase. Further, compound 7b also induced the apoptosis of SMMC-7721 cells in Annexin V-APC/7-AAD binding assay., (Copyright © 2017 Elsevier Ltd. All rights reserved.)- Published
- 2017
- Full Text
- View/download PDF