Synthesis, Cytotoxicity and Anti-Proliferative Activity against AGS Cells of New 3(2H)-Pyridazinone Derivatives Endowed with a Piperazinyl Linker

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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.authoridGallorini, Marialucia/0000-0002-2283-4159
dc.authoridZara, Susi/0000-0003-1705-6943
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidCarradori, Simone/S-4776-2019
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorUysal, Mehtap
dc.contributor.authorCarradori, Simone
dc.contributor.authorGallorini, Marialucia
dc.contributor.authorRicci, Alessia
dc.contributor.authorZara, Susi
dc.date.accessioned2024-08-04T20:49:23Z
dc.date.available2024-08-04T20:49:23Z
dc.date.issued2021
dc.departmentİnönü Üniversitesien_US
dc.description.abstractNovel twenty-three 3(2H)-pyridazinone derivatives were designed and synthesized based on the chemical requirements related to the anti-proliferative effects previously demonstrated within this scaffold. The introduction of a piperazinyl linker between the pyridazinone nucleus and the additional (un)substituted phenyl group led to some compounds endowed with a limited cytotoxicity against human gingival fibroblasts (HGFs) and good anti-proliferative effects against gastric adenocarcinoma cells (AGS) as evaluated by MTT and LDH assays, using doxorubicin as a positive control. Successive analyses revealed that the two most promising representative compounds (12 and 22) could exert their effects by inducing oxidative stress as demonstrated by the hydrogen peroxide release and the morphological changes (cell blebbing) revealed by light microscopy analysis after the haematoxylin-eosin staining. Moreover, to further assess the apoptotic process induced by compounds 12 and 22, Bax expression was measured by flow cytometry. These findings enlarged our knowledge of the structural requirements in this scaffold to display valuable biological effects against cancerous cell lines.en_US
dc.description.sponsorshipMinistero Italiano dell'Universita e della Ricerca (MIUR) [FAR2019]en_US
dc.description.sponsorshipThis work was financed by intramural grants by Ministero Italiano dell'Universita e della Ricerca (MIUR) FAR2019 (ex 60%), held by Simone Carradori.en_US
dc.identifier.doi10.3390/ph14030183
dc.identifier.issn1424-8247
dc.identifier.issue3en_US
dc.identifier.pmid33668893en_US
dc.identifier.scopus2-s2.0-85102245612en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.3390/ph14030183
dc.identifier.urihttps://hdl.handle.net/11616/99807
dc.identifier.volume14en_US
dc.identifier.wosWOS:000634070100001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofPharmaceuticalsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subject3(2H)-pyridazinoneen_US
dc.subjecthydrazoneen_US
dc.subjectfibroblastsen_US
dc.subjectgastric canceren_US
dc.subjectpiperazineen_US
dc.subjectBaxen_US
dc.subjectH2O2 releaseen_US
dc.titleSynthesis, Cytotoxicity and Anti-Proliferative Activity against AGS Cells of New 3(2H)-Pyridazinone Derivatives Endowed with a Piperazinyl Linkeren_US
dc.typeArticleen_US

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