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

KÖPRÜLÜ T. K., Okten S., Tekin S., ÇAKMAK O.

JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, vol.33, no.3, 2019 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 33 Issue: 3
  • Publication Date: 2019
  • Doi Number: 10.1002/jbt.22260
  • Journal Name: JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: apoptosis, cancer cells, cytotoxic activity, nitroquinoline, phenylquinoline, quinolines, 8-SUBSTITUTED QUINOLINES, BROMINATION
  • Yıldız Technical University Affiliated: No

Abstract

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.