Investigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast cancer

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dc.authoridGULCIN, Ilhami -- 0000-0001-5993-1668; Cevik, Ozge -- 0000-0002-9325-3757; orek, cahit -- 0000-0002-3854-1537en_US
dc.contributor.authorDastan, Taner
dc.contributor.authorKocyigit, Umit M.
dc.contributor.authorDastan, Sevgi Durna
dc.contributor.authorKilickaya, Pakize Canturk
dc.contributor.authorTaslimi, Parham
dc.contributor.authorCevik, Ozge
dc.contributor.authorKoparir, Metin
dc.contributor.authorOrek, Cahit
dc.contributor.authorGulcin, Ilhami
dc.contributor.authorCetin, Ahmet
dc.date.accessioned2019-07-27T12:10:23Z
dc.date.accessioned2019-07-28T09:40:02Z
dc.date.available2019-07-27T12:10:23Z
dc.date.available2019-07-28T09:40:02Z
dc.date.issued2017
dc.department[Dastan, Taner -- Cetin, Ahmet] Bingol Univ, Fac Arts & Sci, Div Organ Chem, Dept Chem, TR-12000 Bingol, Turkey -- [Kocyigit, Umit M.] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Dastan, Sevgi Durna] Cumhuriyet Univ, Div Biometry & Genet, Dept Anim Nutr & Zootech, Fac Vet Med, TR-58140 Sivas, Turkey -- [Kilickaya, Pakize Canturk] Cumhuriyet Univ, Sch Pharm, Dept Pharmaceut Biotechnol, TR-58140 Sivas, Turkey -- [Taslimi, Parham -- Gulcin, Ilhami] Ataturk Univ, Dept Chem, Fac Sci, TR-25240 Erzurum, Turkey -- [Cevik, Ozge] Cumhuriyet Univ, Sch Pharm, Dept Biochem, TR-58140 Sivas, Turkey -- [Koparir, Metin -- Orek, Cahit] Firat Univ, Fac Arts & Sci, Div Organ Chem, Dept Chem, TR-23169 Elazig, Turkeyen_US
dc.description.abstractThe aim of this study was to evaluate biologically active novel molecules having potentials to be drugs by their antitumor properties and by activities of apoptotic caspase and topoisomerase. Following syntheses of novel eight bis(-aminoalkyl)phosphinic acid derivatives (4a-h) as a result of array of reactions, compounds were evaluated by cytotoxic effects in vitro on human breast cancer (MCF-7) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF-7 and HUVEC lines, while 4c, 4e, and 4f compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. Also, some of the bis(-aminoalkyl)phosphinic acid derivatives (4a, 4e-h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.en_US
dc.description.sponsorshipCumhuriyet University Research Fund (CUBAP) [V-060]en_US
dc.description.sponsorshipWe acknowledge with great pleasure the partly support provided by Cumhuriyet University Research Fund (CUBAP), project no: V-060.en_US
dc.identifier.doi10.1002/jbt.21971en_US
dc.identifier.issn1095-6670
dc.identifier.issn1099-0461
dc.identifier.issue11en_US
dc.identifier.pmid28833991en_US
dc.identifier.scopus2-s2.0-85033214837en_US
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://dx.doi.org/10.1002/jbt.21971
dc.identifier.urihttps://hdl.handle.net/20.500.12418/6621
dc.identifier.volume31en_US
dc.identifier.wosWOS:000414685200013en_US
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWILEYen_US
dc.relation.ispartofJOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGYen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectacetylcholinesteraseen_US
dc.subjectcytotoxicityen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectphosphinic aciden_US
dc.subjecttopoisomeraseen_US
dc.titleInvestigation of acetylcholinesterase and mammalian DNA topoisomerases, carbonic anhydrase inhibition profiles, and cytotoxic activity of novel bis(-aminoalkyl)phosphinic acid derivatives against human breast canceren_US
dc.typeArticleen_US

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