Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages

Gurkan A. S., KARABAY A. Z., Buyukbingol Z., Buyukbingol E.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.46, sa.2, ss.468-479, 2011 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 46 Sayı: 2
  • Basım Tarihi: 2011
  • Doi Numarası: 10.1016/j.ejmech.2010.11.021
  • Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.468-479
  • Anahtar Kelimeler: Nitric oxide, RAW 264.7 macrophage cells, Retinoids, Tempamine, TRANS-RETINOIC ACID, ANTIOXIDANT ACTIVITY, BIOLOGICAL EVALUATION, LIPOIC ACID, IN-VITRO, DESIGN, PROOXIDANT, NITROXIDE, CYTOKINES, CELLS
  • Ankara Üniversitesi Adresli: Evet

Özet

In this study, novel N-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalene-2-yl)-carboxamide (6-15) and 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide (16-32) derivatives were synthesized and their in vitro effects at 5 mu M and 50 mu M concentrations on proliferation and nitric oxide (NO center dot) production in lipopolysaccharide (LPS) activated RAW 264.7 macrophage cells were determined. Compounds 12, 17, 24 and 26 were found to decrease nitrite levels in a dose-dependent manner in LPS-activated cells. At the tested concentrations, these compounds did not exhibit cytotoxic effects. Interestingly, compound 27 which contains nitroxide free radical was the most active compound in this series showing 59.2% nitrite inhibition in LPS-activated macrophage cells. (C) 2010 Elsevier Masson SAS. All rights reserved.