Title:6-Chloro-7-methyl-3', 4'-dimethoxyflavone – a Potent Selective COX-2 Inhibitor
VOLUME: 9 ISSUE: 4
Author(s):Rafia Bashir, Kalim Javed, Shafiya Yaseen, Syed Ovais, Pooja Rathore, Hinna Hamid, M. S. Alam, Mohammed Samim, Surender Singh and Vinod Nair
Affiliation:Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India.
Keywords:Chalcones, flavones, anti-inflammatory activity, selective COX-2 inhibitor
Abstract:Some unnatural chalcones (1a-q) and flavones (2a-d) have been synthesized and evaluated for their antiinflammatory
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.
