Synthesis and bioactivity studies on new 4-(3-(4-Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2-c]pyrazol-2-yl) benzenesulfonamides
| Autor: | Claudiu T. Supuran, Parham Taslimi, Halise Inci Gul, Mehtap Tugrak, Hiroshi Sakagami, İlhami Gülçin |
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| Přispěvatelé: | Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü |
| Rok vydání: | 2016 |
| Předmět: |
Spectrometry
Mass Electrospray Ionization Stereochemistry Cytotoxicity Proton Magnetic Resonance Spectroscopy Indane Tumor selectivity Pyrazole Benzenesulfonamide 01 natural sciences Inhibitory Concentration 50 chemistry.chemical_compound Cell Line Tumor Carbonic anhydrase Drug Discovery Humans Inhibitory concentration 50 Carbon-13 Magnetic Resonance Spectroscopy Pharmacology Sulfonamides biology 010405 organic chemistry Chemistry General Medicine 0104 chemical sciences 010404 medicinal & biomolecular chemistry Carbonic anhydrase/enzyme inhibition biology.protein |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 31:1619-1624 |
| ISSN: | 1475-6374 1475-6366 |
| DOI: | 10.3109/14756366.2016.1160077 |
| Popis: | A series of new 4-(3-(4-substitutedphenyl)-3a, 4-dihydro-3H-indeno[1,2-c] pyrazol-2-yl) benzenesulfonamides (7-12) was synthesized starting from 2-(4-substitutedbenzylidene)-2,3-dihydro-1H-inden-1-one (1-6) and 4-hydrazinobenzenesulfonamide. The substituted benzaldehydes from which the key intermediate was prepared by introducing 2- or 4-substituents such as fluorine, hydroxy, methoxy, or the 3,4,5-trimethoxy moieties. The compounds were tested for their cytotoxicity, tumor-specificity and potential as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The 3,4,5-trimethoxy and the 4-hydroxy derivatives showed interesting cytotoxic activities, which may be crucial for further anti-tumor activity studies, whereas some of these sulfonamides strongly inhibited both human (h) cytosolic isoforms hCA I and II. |
| Databáze: | OpenAIRE |
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