Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents
| Autor: | Rengul Cetin-Atalay, Sultan Nacak Baytas, Nazan Inceler, Deniz Cansen Kahraman, Nilüfer N. Turan, Yeşim Özkan |
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| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Pharmacology chemistry.chemical_classification biology Chemistry Organic Chemistry Pharmaceutical Science Biochemistry 3. Good health 03 medical and health sciences 030104 developmental biology 0302 clinical medicine Enzyme Design synthesis Cell culture 030220 oncology & carcinogenesis Drug Discovery biology.protein Molecular Medicine Cytotoxic T cell Cyclooxygenase Human cancer Biological evaluation |
| Popis: | With the aim of achieving new compounds possessing both anti-inflammatory and antiplatelet activities, we synthesized (E)-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides, and evaluated their COX-1 and COX-2 inhibitory and antiplatelet activities. Since COX-2 inhibitory and antiplatelet compounds have anticancer potential, we also screened their antiproliferative effects against three human cancer cell lines. Compounds 5n, 5p, 5s, 10d, 10g and 10i were determined as dual COX-2 inhibitor/antiplatelet compounds. Compound 10h appeared to be a compound that exhibited antiplatelet activity without inhibiting the COX enzyme. Compounds 5h, 10a and 10i were the most effective derivatives which displayed antiproliferative activity against Huh7, MCF7 and HCT116 cells. Particularly, compound 10i, as the compound exhibiting the highest cytotoxic, antiplatelet and COX-2 inhibitory activity, was remarkable. |
| Databáze: | OpenAIRE |
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