6-Chloro-7-methyl-3′, 4′-dimethoxyflavone - a Potent Selective COX-2 Inhibitor

被引：1

作者：

Bashir, Rafia ^{[1
]}

Javed, Kalim ^{[1
]}

Yaseen, Shafiya ^{[1
]}

Ovais, Syed ^{[1
]}

Rathore, Pooja ^{[1
]}

Hamid, Hinna ^{[1
]}

Alam, M. S. ^{[1
]}

Samim, Mohammed ^{[1
]}

Singh, Surender ^{[2
]}

Nair, Vinod ^{[2
]}

机构：

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

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

来源：

MEDICINAL CHEMISTRY | 2013年 / 9卷 / 04期

关键词：

Chalcones; flavones; anti-inflammatory activity; selective COX-2 inhibitor; OVER-EXPRESSION; CANCER-CELL; FLAVONOIDS; CYCLOOXYGENASE-2; CHALCONES;

D O I：

10.2174/1573406411309040016

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Some unnatural chalcones (1a-q) and flavones (2a-d) have been synthesized and evaluated for their anti-inflammatory activity using carrageenan-induced rat paw edema assay. The flavone 2c (6-Chloro-7-methyl-3', 4'-dimethoxyflavone) had higher anti-inflammatory activity and superior gastrointestinal safety profiles than the reference drug celecoxib. Compound 2c showed almost two times better selective inhibitory activity towards COX-2 enzyme than celecoxib. 2'-Hydroxychalcones (1a-h) showed moderate to strong anti-inflammatory activity (38.6-82.4 % at 3h and 52.4-80.2 % at 5h). Among 2'-methoxychalcones (1i-q) 1k and 1q exhibited maximum activity 82.6% (at 3h) and 84.3% (at 5h) respectively.

引用

页码：617 / 623

页数：7

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