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Synthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells

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dc.contributor.authorÖZSAVCI, DERYA
dc.contributor.authorsKucukguzel, S. Guniz; Koc, Derya; Cikla-Suzgun, Pelin; Ozsavci, Derya; Bingol-Ozakpinar, Ozlem; Mega-Tiber, Pinar; Orun, Oya; Erzincan, Pinar; Sag-Erdem, Safiye; Sahin, Fikrettin
dc.date.accessioned2022-03-13T12:49:42Z
dc.date.available2022-03-13T12:49:42Z
dc.date.issued2015
dc.description.abstractTolmetin hydrazide and a novel series of tolmetin hydrazide-hydrazones 4a-l were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, H-1 NMR) methods. N-[(2,6-Dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) was evaluated in vitro using the MTT colorimetric method against the colon cancer cell lines HCT-116 (ATCC, CCL-247) and HT-29 (ATCC, HTB-38) to determine growth inhibition and cell viability at different doses. Compound 4g exhibited anti-cancer activity with an IC50 value of 76M against colon cancer line HT-29 (ATCC, HTB-38) and did not display cytotoxicity toward control NIH3T3 mouse embryonic fibroblast cells compared to tolmetin. In addition, this compound was evaluated for caspase-3, caspase-8, caspase-9, and annexin-V activation in the apoptotic pathway, which plays a key role in the treatment of cancer. We demonstrated that the anti-cancer activity of this compound was due to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway. In addition, in this study, we investigated the catalytical effect of COX on the HT-29 cancer line, the apoptotic mechanism, and the moleculer binding of tolmetin and compound 4g on the COX enzyme active site.
dc.identifier.doi10.1002/ardp.201500178
dc.identifier.eissn1521-4184
dc.identifier.issn0365-6233
dc.identifier.pubmed26287512
dc.identifier.urihttps://hdl.handle.net/11424/238299
dc.identifier.wosWOS:000362565600005
dc.language.isoeng
dc.publisherWILEY-V C H VERLAG GMBH
dc.relation.ispartofARCHIV DER PHARMAZIE
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectApoptosis
dc.subjectCaspase-3
dc.subjectColon cancer
dc.subjectHydrazide-hydrazone
dc.subjectTolmetin
dc.subjectNONSTEROIDAL ANTIINFLAMMATORY DRUGS
dc.subjectCOLORECTAL-CANCER
dc.subjectANTI-HCV
dc.subjectBIOLOGICAL-ACTIVITIES
dc.subjectPRO-APOPTOSIS
dc.subjectASPIRIN USE
dc.subjectIN-VITRO
dc.subjectCOX-2
dc.subjectDERIVATIVES
dc.subjectANTICANCER
dc.titleSynthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells
dc.typearticle
dspace.entity.typePublication
local.avesis.id914ba04f-ff71-41d9-bcfb-470ee3327429
local.import.packageSS17
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.numberofpages13
oaire.citation.endPage742
oaire.citation.issue10
oaire.citation.startPage730
oaire.citation.titleARCHIV DER PHARMAZIE
oaire.citation.volume348
relation.isAuthorOfPublication68ec1222-da29-4568-a8e5-56ebd6b48020
relation.isAuthorOfPublication.latestForDiscovery68ec1222-da29-4568-a8e5-56ebd6b48020

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