Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives

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Gurkan-Alp A. S., Mumcuoglu M., Andac C. A., Dayanc E., Cetin-Atalay R., Buyukbingol E.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.58, ss.346-354, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 58
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1016/j.ejmech.2012.10.013
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.346-354
  • Anahtar Kelimeler: Indole, MDA-MB-231, Molecular dynamics, Retinoid, T47D, ANTITUMOR-ACTIVITY, ACID RECEPTORS, BREAST-CANCER, EXPRESSION, CHEMOPREVENTION, SIMULATION, INHIBITOR, APOPTOSIS, SUBTYPES, SOLVENT
  • Ankara Üniversitesi Adresli: Evet

Özet

In this study, novel (E)-3-(5-substituted-1H-indol-3-yl)-1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-2-en-1-one (5(a-e)) derivatives were synthesized and their anticancer effects were determined in vitro. Novel indole retinoid compounds except Se have anti-proliferative capacity in liver, breast and colon cancer cell lines. This anti-proliferative effect was further analyzed in breast cancer cell line panel by using the most potent compound Sa. It was determined that 5a can inhibit proliferation at very low IC50 concentrations in all of the breast cancer cell lines. Here, we present some evidence on apoptotic termination of cancer cell proliferation which may be primarily driven by the inhibition of RXR alpha and, to a lesser extent, RXR gamma. (C) 2012 Elsevier Masson SAS. All rights reserved.