1. Synthesis and Biological Evaluation of New Phthalazinone Derivatives as Anti-Inflammatory and Anti-Proliferative Agents
- Author
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Alhamzah Dh. Hameed, Mohammed Samim, Mymona Akhtar, Surender Singh, Kalicharan Sharma, Kalim Javed, Raed Yaseen, Pooja Rathore, and Syed Ovais
- Subjects
0301 basic medicine ,Drug ,medicine.drug_class ,Chemistry ,media_common.quotation_subject ,Pharmaceutical Science ,Nanotechnology ,Carbon-13 NMR ,Pharmacology ,Anti-inflammatory ,In vitro ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,0302 clinical medicine ,In vivo ,030220 oncology & carcinogenesis ,Drug Discovery ,medicine ,Proton NMR ,Phthalazine ,Etoricoxib ,medicine.drug ,media_common - 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.
- Published
- 2016