Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells

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dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridCarradori, Simone/0000-0002-8698-9440
dc.authoridDi Simone, Simonetta Cristina/0000-0001-5041-3848
dc.authoridUTKU, Semra/0000-0003-3181-9134
dc.authoridReis, AlessanRSS/0000-0001-8486-7469
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.authorwosid, Claudio/GLU-3638-2022
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidCarradori, Simone/S-4776-2019
dc.authorwosidFerrante, Claudio/AEY-9584-2022
dc.authorwosidUTKU, Semra/F-7927-2015
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorUtku, Semra
dc.contributor.authorMathew, Bijo
dc.contributor.authorCarradori, Simone
dc.contributor.authorOrlando, Giustino
dc.contributor.authorDi Simone, Simonetta
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.date.accessioned2024-08-04T20:47:15Z
dc.date.available2024-08-04T20:47:15Z
dc.date.issued2020
dc.departmentİnönü Üniversitesien_US
dc.description.abstractNovel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 mu g/mL for all compounds. Successive assays revealed that some compounds were endowed with a promising anti-proliferative effect against HCT116 cells, alone or stimulated by serotonin as a pro-inflammatory factor in order to mimick an inflamed model in vivo of cancer cell microenvironment. Moreover, the kinurenic acid level after treatment with these newly synthesised compounds was monitored as a marker of anti-proliferation in colon carcinoma models. The IC50 values obtained for the best-in-class compounds were comparable to that of daunorubicin as a reference drug. Conversely, these compounds were not able to counteract the spontaneous migration of human cancer HCT116 cell line in the wound healing paradigm.en_US
dc.description.sponsorshipMinistero Italiano dell'Universita e della Ricerca (MIUR) FAR 2019en_US
dc.description.sponsorshipThis work was supported by intramural grants by Ministero Italiano dell'Universita e della Ricerca (MIUR) FAR 2019 (ex 60%), held by Dr. Simone Carradori.en_US
dc.identifier.doi10.1080/14756366.2020.1755670
dc.identifier.endpage1109en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue1en_US
dc.identifier.pmid32321320en_US
dc.identifier.scopus2-s2.0-85083782939en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1100en_US
dc.identifier.urihttps://doi.org/10.1080/14756366.2020.1755670
dc.identifier.urihttps://hdl.handle.net/11616/99261
dc.identifier.volume35en_US
dc.identifier.wosWOS:000527814500001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectSerotoninen_US
dc.subjectanti-proliferative agentsen_US
dc.subjectpyridazinoneen_US
dc.subjectkynurenic aciden_US
dc.subjectHCT116en_US
dc.subjectwound healingen_US
dc.subjectArtemia salina lethality testen_US
dc.titleSynthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cellsen_US
dc.typeArticleen_US

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