Synthesis and anti-inflammatory activity of celecoxib like compounds
| Autor: | Syed Ovais, Vinod Nair, Rafia Bashir, Mohammed Samim, Surender Singh, Kalim Javed, Pooja Rathore, Shafiya Yaseen |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
medicine.drug_class
Analgesic Antineoplastic Agents Pyrazoline Pharmacology Carrageenan Nitric Oxide Anti-inflammatory Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Edema Humans Cell Proliferation Sulfonamides Dose-Response Relationship Drug Molecular Structure Tumor Necrosis Factor-alpha Melanoma Anti-Inflammatory Agents Non-Steroidal General Medicine Reference drug medicine.disease Rats chemistry Celecoxib Cell culture Prostaglandins Pyrazoles Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry. 28:1105-1112 |
| ISSN: | 1475-6374 1475-6366 |
| Popis: | Nine novel 4-[3-(4-Dimethylamino-phenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]-benzenesulfonamides (2a-i) were synthesized and evaluated for their anti-inflammatory and antiproliferative activities. These compounds (2a-i) showed moderate to strong anti-inflammatory activity in carrageenan rat paw oedema test. Compounds 2b, 2d and 2g showing comparable anti-inflammatory activity to that of reference drug celecoxib were evaluated for their ulcerogenic and analgesic activities. The effect of 2b, 2d and 2g on the content of NO, TNF-α and PGE2 in exudates from rat paw stimulated by carrageenan was also evaluated. The compound 2c showed considerable antitumor activities against all 60 human tumor cell lines with effective GI50 (MG-MID) value of 3.63 µM. It exhibited maximum activity against melanoma (LOX IMVI and SK-MEL-5) cancer cell lines with GI50 value less than 2 μM. |
| Databáze: | OpenAIRE |
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