Synthesis and anti-inflammatory activity of celecoxib like compounds. (1st October 2013)

• Record Type: Journal Article
• Authors: Ovais, Syed; Yaseen, Shafiya; Bashir, Rafia; Rathore, Pooja; Samim, Mohammed; Singh, Surender; Nair, Vinod; Javed, Kalim
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 28:Number 5(2013:Oct.)
• Page Start: 1105
• Page End: 1112
• Publication Date: 2013-10-01
• Subjects: Pyrazoline -- tumor necrosis factor (TNF-α) -- prostaglandin E2 (PGE2) -- nitrite (NO) -- antiproliferative activity; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2012.710847
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract : 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. Compounds2b, 2d and2g showing comparable anti-inflammatory activity to that of reference drug celecoxib were evaluated for their ulcerogenic and analgesic activities. The effect of2b, 2d and2g on the content of NO, TNF-α and PGE2 in exudates from rat paw stimulated by carrageenan was also evaluated. The compound2c 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.