Biological Activity of 1-Aryl-3-phenethylamino-1-propanone Hydrochlorides and 3-Aroyl-4-aryl-1-phenethyl-4-piperidinols on PC-3 Cells and DNA Topoisomerase I Enzyme

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dc.contributor.authorMete, Ebru
dc.contributor.authorGul, Halise Inci
dc.contributor.authorCanturk, Pakize
dc.contributor.authorTopcu, Zeki
dc.contributor.authorPandit, Bulbul
dc.contributor.authorGul, Mustafa
dc.contributor.authorLi, Pui-Kai
dc.date.accessioned2019-10-27T21:14:16Z
dc.date.available2019-10-27T21:14:16Z
dc.date.issued2010
dc.departmentEge Üniversitesien_US
dc.description.abstractA number of studies reported Mannich bases to manifest antimicrobial, cytotoxic, anticancer, anti-inflammatory, and anticonvulsant activities. A considerable number of therapeutically important cytotoxic compounds are active on DNA topoisomerases that regulate the DNA topology. In the present study we evaluated the biological activity of mono-Mannich bases, 1-aryl-3-phenethylamino-1-propanone hydrochlorides (1a-10a), and semicyclic mono-Mannich bases, 3-aroyl-4-aryl-1-phenethyl-4-piperidinols (1b-9b), synthesized in our laboratory. We employed androgen-independent human prostate cancer cells (PC-3) to assess the cytotoxicity of the compounds and extended the biological activity evaluation to cover supercoil relaxation assays of mammalian type I topoisomerases. Our results showed that the compounds had cytotoxicity within the 8.2-32.1 mu m range, while two compounds gave rise to a comparable average value in topo I interference of 42% and 40% for 10a (with a hydroxy substituent on the phenyl ring from mono-Mannich bases) and 5b (with a fluoro substituent on the phenyl ring from the semicyclic mono-Mannich base series, piperidinols), respectively.en_US
dc.description.sponsorshipScientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TBAG108T548]; Research Foundation of Ataturk University, Erzurum, TurkeyAtaturk University [2006/96, 2007/225]en_US
dc.description.sponsorshipThis study was supported by grants from The Scientific and Technological Research Council of Turkey (Grant No. TBAG108T548) to Z. T. and from Research Foundation of Ataturk University, Erzurum, Turkey (Grant No. 2006/96, 2007/225) to H. I. G. The authors thank Dr. Mustafa Arik for the calculations of the Log P values.en_US
dc.identifier.endpage652en_US
dc.identifier.issn0939-5075
dc.identifier.issn1865-7125
dc.identifier.issue11.Decen_US
dc.identifier.pmid21319705en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage647en_US
dc.identifier.urihttps://hdl.handle.net/11454/43355
dc.identifier.volume65en_US
dc.identifier.wosWOS:000288580900003en_US
dc.identifier.wosqualityQ4en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWalter De Gruyter Gmbhen_US
dc.relation.ispartofZeitschrift Fur Naturforschung Section C-A Journal of Biosciencesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectMono-Mannich Basesen_US
dc.subjectCytotoxic Activityen_US
dc.subjectPC-3 Cellen_US
dc.subjectDNA Topoisomerase Ien_US
dc.titleBiological Activity of 1-Aryl-3-phenethylamino-1-propanone Hydrochlorides and 3-Aroyl-4-aryl-1-phenethyl-4-piperidinols on PC-3 Cells and DNA Topoisomerase I Enzymeen_US
dc.typeArticleen_US

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