A SAR Study: Evaluation of Bromo Derivatives of 8-Substituted Quinolines as Novel Anticancer Agents


Okten S., Cakmak O. , Tekin S., Koprulu T. K.

LETTERS IN DRUG DESIGN & DISCOVERY, vol.14, no.12, pp.1415-1424, 2017 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 14 Issue: 12
  • Publication Date: 2017
  • Doi Number: 10.2174/1570180814666170504150050
  • Title of Journal : LETTERS IN DRUG DESIGN & DISCOVERY
  • Page Numbers: pp.1415-1424
  • Keywords: SAR, bromination, hydroxyquinoline, methoxyquinoline, cyanoquinoline, anticancer effect, cytotoxicity, antitopoisomerase, 8-HYDROXYQUINOLINE, INHIBITORS

Abstract

Background: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5,7-Dibromo-5, 7-bromo-6, 7-cyano-11 and 5,7-dicyano-12 8-hydroxyquinolines were shown to have strong antiproliferative activity against various tumor cell lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) with IC50 values ranged from 6.7 to 25.6 mu g/mL.