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Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities
Faculty
Pharmacy
Year:
2021
Type of Publication:
ZU Hosted
Pages:
Authors:
Hend Kather Abdelhakem Elhamalawy
Staff Zu Site
Abstract In Staff Site
Journal:
Journal of Enzyme Inhibition and Medicinal Chemistry Taylor &Francis
Volume:
Keywords :
Design , synthesis , novel quinazolinones conjugated ibuprofen, indole
Abstract:
Novel quinazolinones conjugated with indole acetamide (4a–c), ibuprofen (7a–e), or thioacetohydrazide (13a,b, and 14a-d) were designed to increase COX-2 selectivity. The three synthesised series exhibited superior COX-2 selectivity compared with the previously reported quinazolinones and their NSAID analogue and had equipotent COX-2 selectivity as celecoxib. Compared with celecoxib, 4b, 7c, and 13 b showed similar anti-inflammatory activity in vivo, while 13 b and 14a showed superior inhibition of the inflammatory mediator nitric oxide, and 7 showed greater antioxidant potential in macrophages cells. Moreover, all selected compounds showed improved analgesic activity and 13 b completely abolished the pain response. Additionally, compound 4a showed anticancer activity in tested cell lines HCT116, HT29, and HCA7. Docking results were consistent with COX-1/2 enzyme assay results. In silico studies suggest their high oral bioavailability. The overall findings for compounds (4a,b, 7c, 13 b, and 14c) support their potential role as anti-inflammatory agents.
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Hend Kather Abdelhakem Elhamalawy, "Preclinical evaluation of Rad6 inhibition to overcome platinum resistance in ovarian cancer", AACR, 2016
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Hend Kather Abdelhakem Elhamalawy, "Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides", ELSEVIER, 2013
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Hend Kather Abdelhakem Elhamalawy, "Synthesis of New 2,3-Dihydroquinazolin-4(1H)-one Derivatives for Analgesic and Anti-inflammatory Evaluation", WILEY interscience, 2010
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Hend Kather Abdelhakem Elhamalawy, "Synthesis of new benzotriazepin-5(2H)-one derivatives of expected antipsychotic activity", springer link, 2013
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Hend Kather Abdelhakem Elhamalawy, "Novel Inhibitors of Rad6 Ubiquitin Conjugating Enzyme: Design, Synthesis, Identification, and Functional Characterization", AACR publications, 2013
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Department Related Publications
Abdallah Ahmed Abdallah Elshanawany, "Development and validation of liquid chromatographic method for simultaneous determination of amiloride hydrochloride and hydrochlorothiazide in human urine", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "HPLC Determination of polymyxin sulphate, Benzalkonium chloride, and gramicidine in pharm.formulation ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Synchronous Spectroflurimetric Determination of Famtidine,Fluconazole and Ketoconazole in bulk powder and in pharmaceutical dosages forms ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Synthesis of 3- substituted (6-bromo-2-imidazo{4,5-b}pyridinyl)propionic acid as antiinflammatory agents. ", لايوجد, 1900
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Abdallah Ahmed Abdallah Elshanawany, "Application of difference spectrophotometry to the nitrosation reaction in the assay of certain antipyretic drugs . ", لايوجد, 1900
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