Synthesis of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide as anticancer and anti-inflammatory agents |
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Authors: | Bashir Rafia Ovais Syed Yaseen Shafiya Hamid Hinna Alam M S Samim Mohammad Singh Surender Javed Kalim |
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Institution: | a Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi 110 062, India b Department of Pharmacology, All India Institute of Medical Sciences, New Delhi 110 029, India |
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Abstract: | Thirteen new 2-pyrazoline derivatives bearing benzenesulfonamide moiety (2a-m) were synthesized by condensing appropriate chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anticancer and anti-inflammatory actions. According to the protocol of the National Cancer Institute (NCI) in vitro disease-oriented human cells screening panel assay compounds 2b, 2c, 2e, 2f and 2g exhibited considerable antitumor activities against the entire tested tumor cell lines and showed effective growth inhibition GI50 (MG-MID) values of 2.63, 2.57, 6.61, 3.31 and 2.57 μM, respectively, beside a cyclostatic activity TGI (MG-MID) 9.54, 8.51, 24.0, 19.9 and 8.71 μM, respectively. Two compounds 2g and 2k showed more potent anti-inflammatory activity than celecoxib at 5 h in carrageenan-induced rat paw edema bioassay. These compounds (2g and 2k) proved to have superior gastrointestinal safety profiles as compared to celecoxib, when tested for their ulcerogenic effects. Compounds 2g and 2k showed no inhibition against the enzymatic activity of bovine COX-2 (in vitro). |
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Keywords: | 2-Pyrazolines Anti-inflammatory activity Ulcerogenic activity Cyclooxygenase activity Celecoxib |
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