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Synthesis, molecular docking and biological evaluation of quinolone derivatives as novel anticancer agents.

Authors
  • Li, Jie1
  • Zheng, Tu-Cai1
  • Jin, Yi1
  • Xu, Jian-Guo1
  • Yu, Jian-Gang1
  • Lv, Yan-Wen1
  • 1 College of Chemistry and Materials Engineering, Quzhou University.
Type
Published Article
Journal
Chemical and Pharmaceutical Bulletin
Publisher
Pharmaceutical Society of Japan
Publication Date
Nov 09, 2017
Identifiers
DOI: 10.1248/cpb.c17-00035
PMID: 29118308
Source
Medline
Keywords
License
Unknown

Abstract

A series of novel quinolone derivatives (8a-j) were synthesized, and their anticancer activities were tested in human cancer cell lines A549, HL-60, and Hela. Compound 8i was found to be 5-times more potent in cell-killing activity for cell lines A549, HL-60, and Hela than the positive control irinotecan or cisplatin, with IC50 of 0.009, 0.008 and 0.010 μM, respectively. The docking study revealed that compound 8i might have strong interactions with the active site of DNA-Topoisomerase I.

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