Biological evaluation of some quinoline derivatives with different functional groups as anticancer agents

J Biochem Mol Toxicol. 2019 Mar;33(3):e22260. doi: 10.1002/jbt.22260. Epub 2018 Nov 15.


Due to a great deal of biological activities, quinoline derivatives have drawn attention for synthesis and biological activities in the search for new anticancer drug development. In this work, a variety of substituted (phenyl, nitro, cyano, N-oxide, and methoxy) quinoline derivatives (3-13) were tested in vitro for their biological activity against cancer cell lines, including rat glioblastoma (C6), human cervical cancer cells (HeLa), and human adenocarcinoma (HT29). 6-Bromo-5-nitroquinoline (4), and 6,8-diphenylquinoline (compound 13) showed the greatest antiproliferative activity as compared with the reference drug, 5-fluorouracil (5-FU), while the other compounds showed low antiproliferative activity. 6-Bromo-5-nitroquinoline (4) possesses lower cytotoxic activity than 5-FU in HT29 cell line. Due to its the apoptotic activity 6-Bromo-5-nitroquinoline (4) has the potential to cause cancer cell death.

Keywords: apoptosis; cancer cells; cytotoxic activity; nitroquinoline; phenylquinoline; quinolines.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Drug Screening Assays, Antitumor
  • HeLa Cells
  • Humans
  • Nitro Compounds / pharmacology*
  • Quinolines / pharmacology*
  • Rats


  • Antineoplastic Agents
  • Nitro Compounds
  • Quinolines