Synthesis and anti-inflammatory activity of celecoxib like compounds

被引：11

作者：

Ovais, Syed ^{[1
]}

Yaseen, Shafiya ^{[1
]}

Bashir, Rafia ^{[1
]}

Rathore, Pooja ^{[1
]}

Samim, Mohammed ^{[1
]}

Singh, Surender ^{[2
]}

Nair, Vinod ^{[2
]}

Javed, Kalim ^{[1
]}

机构：

[1] Jamia Hamdard, Dept Chem, Fac Sci, New Delhi 110062, India

[2] All India Inst Med Sci, Dept Pharmacol, New Delhi, India

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2013年 / 28卷 / 05期

关键词：

Pyrazoline; tumor necrosis factor (TNF-alpha); prostaglandin E2 (PGE2); nitrite (NO); antiproliferative activity; BEARING BENZENE SULFONAMIDE; NATIONAL-CANCER-INSTITUTE; PYRAZOLINE DERIVATIVES; CARBONIC-ANHYDRASE; DRUG DISCOVERY; ANALGESIC AGENTS; ANTICANCER; INHIBITORS; DESIGN; SCREEN;

D O I：

10.3109/14756366.2012.710847

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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-alpha and PGE(2) 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 GI(50) (MG-MID) value of 3.63 mu M. It exhibited maximum activity against melanoma (LOX IMVI and SK-MEL-5) cancer cell lines with GI(50) value less than 2 mu M.

引用

页码：1105 / 1112

页数：8

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