Synthesis and evaluation of new indole-based chalcones as potential antiinflammatory agents
| Autor: | Mehlika Dilek Altıntop, Ahmet Özdemir, Ozkan Alatas, Gülhan Turan-Zitouni, Gülşen Akalın Çiftçi, Zafer Asım Kaplancıklı, İpek Ertorun |
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| Přispěvatelé: | Anadolu Üniversitesi, Eczacılık Fakültesi, Farmasötik Kimya Anabilim Dalı, Özdemir, Ahmet, Altıntop, Mehlika Dilek, Turan, Gülhan, Çiftçi, Gülsen Akalın, Kaplancıklı, Zafer Asım |
| Rok vydání: | 2014 |
| Předmět: |
Chalcone
Antioxidant Indoles Cell Survival medicine.medical_treatment Drug Evaluation Preclinical Mouse embryonic fibroblast chemistry.chemical_compound Mice Chalcones Liver Function Tests Sepsis Drug Discovery medicine Cytotoxic T cell Animals Cyclooxygenase Inhibitors Pharmacology Indole test biology Molecular Structure Chemistry Organic Chemistry Membrane Proteins General Medicine Cyclooxygenase Disease Models Animal Oxidative Stress COX Inhibitor Biochemistry Indole Cyclooxygenase 2 Drug Design biology.protein Cyclooxygenase 1 NIH 3T3 Cells Lipid Peroxidation |
| Zdroj: | European journal of medicinal chemistry. 89 |
| ISSN: | 1768-3254 0003-4800 |
| Popis: | WOS: 000348003500027 PubMed ID: 25462246 In the present work, new indole-based chalcone derivatives were obtained via the reaction of 5-substituted-1H-indole-3-carboxaldehydes/1-methylindole-3-carboxaldehyde with appropriate acetophenones. The synthesized compounds were investigated for their in vitro COX-1 and COX-2 inhibitory activity. The most effective COX inhibitors were also evaluated for their in vivo antiinflammatory and antioxidant activities in LPS induced sepsis model. Furthermore, the CCK-8 assay was carried out to determine cytotoxic effects of all compounds against NIH/3T3 mouse embryonic fibroblast cells. 3-(5-Bromo-1H-indol-3-yl)-1-(4-cyanophenyl)prop-2-en-1-one (6) can be considered as a non-selective COX inhibitor (COX-1 IC50 = 8.1 +/- 0.2 mu g/mL, COX-2 IC50 = 9.5 +/- 0.8 mu g/mL), whereas 3-(5-methoxy-1H-indol-3-yl)-1-(4-(methylsulfonyl)phenyl)prop-2-en-1-one (1) inhibited only COX-1 (IC50 = 8.6 +/- 0.1 mu g/mL). According to in vivo studies, these compounds also displayed antiinflammatory and antioxidant activities Anadolu University Scientific Research Projects Commission [1306S227] This study was supported by Anadolu University Scientific Research Projects Commission under the grant no: 1306S227. |
| Databáze: | OpenAIRE |
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