title: Synthesis and anti-inflammatory activity of celecoxib like compounds.
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. 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-α and PGE2 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 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.
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University) , New Delhi , India.
authors.forename: Syed
authors.initials: S
authors.lastname: Ovais
authors.forename: Shafiya
authors.initials: S
authors.lastname: Yaseen
authors.forename: Rafia
authors.initials: R
authors.lastname: Bashir
authors.forename: Pooja
authors.initials: P
authors.lastname: Rathore
authors.forename: Mohammed
authors.initials: M
authors.lastname: Samim
authors.forename: Surender
authors.initials: S
authors.lastname: Singh
authors.forename: Vinod
authors.initials: V
authors.lastname: Nair
authors.forename: Kalim
authors.initials: K
authors.lastname: Javed
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002351:Carrageenan; D000068579:Celecoxib; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D006801:Humans; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D011453:Prostaglandins / Q000096:biosynthesis / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D011453:Prostaglandins; D011720:Pyrazoles; D013449:Sulfonamides; D014409:Tumor Necrosis Factor-alpha; D009569:Nitric Oxide; D002351:Carrageenan; D000068579:Celecoxib