title: Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents.
abstract: The chemistry of phthalazine derivatives has been of increasing interest since many of these compounds have found many chemotherapeutic applications. So this study aims to synthesize a library of phthalazine derivatives and to investigate their anti-inflammatory and anti-proliferative activities. Sixteen new phthalazinone derivatives (2a-p) were synthesized and tested for their in vitro antiproliferative and in vivo anti-inflammatory activities. All the synthesized compounds were identified and characterized by IR, (1) H NMR, (13) C NMR spectroscopy, and MS. Two compounds, 2b and 2i, showed significant anti-inflammatory activity comparable with that of the standard drug etoricoxib in the carrageenan-induced rat paw edema model at 3 and 5 h, respectively. Three compounds (2h, 2j, and 2g) showed moderate sensitivity toward the renal cancer cell line UO-31.
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Alhamzah Dh
authors.initials: AD
authors.lastname: Hameed
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.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Raed
authors.initials: R
authors.lastname: Yaseen
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Pooja
authors.initials: P
authors.lastname: Rathore
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Samim
authors.affiliation: Department of Pharmacology, All India Institute of Medical Science, New Delhi, India.
authors.forename: Surender
authors.initials: S
authors.lastname: Singh
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Drug Design and Medicinal Chemistry Laboratory, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Kalicharan
authors.initials: K
authors.lastname: Sharma
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Drug Design and Medicinal Chemistry Laboratory, Jamia Hamdard (Hamdard University), New Delhi, India.
authors.forename: Mymona
authors.initials: M
authors.lastname: Akhtar
authors.affiliation: Department of Chemistry, Faculty of Science, Jamia Hamdard (Hamdard University), New Delhi, India.
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; D045744:Cell Line, Tumor; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005260:Female; D006801:Humans; D008297:Male; D010793:Phthalazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C000613239:2-(4-methanesulfonylphenyl)-4-(5,6,7,8-tetrahydronaphthalen-2-yl)phthalazin-1-one; C000613238:4-(4-biphenyl)-2-(4-(methylsulfonyl)phenyl)phthalazin-1(2H)-one; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D052246:Cyclooxygenase 2 Inhibitors; D010793:Phthalazines; D013450:Sulfones; D002351:Carrageenan
keywords: Anti-inflammatory activity; Anti-proliferative activity; COX-2; LOX-5 inhibitors; Phthalazone