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, cilt.14, sa.12, ss.1415-1424, 2017 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 14 Sayı: 12
  • Basım Tarihi: 2017
  • Doi Numarası: 10.2174/1570180814666170504150050
  • Dergi Adı: LETTERS IN DRUG DESIGN & DISCOVERY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1415-1424
  • Anahtar Kelimeler: SAR, bromination, hydroxyquinoline, methoxyquinoline, cyanoquinoline, anticancer effect, cytotoxicity, antitopoisomerase, 8-HYDROXYQUINOLINE, INHIBITORS
  • Yıldız Teknik Üniversitesi Adresli: Hayır

Özet

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.