Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity

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dc.contributor.authorCalogeropoulou, T.en
dc.contributor.authorAvlonitis, N.en
dc.contributor.authorMinas, V.en
dc.contributor.authorAlexi, X.en
dc.contributor.authorPantzou, A.en
dc.contributor.authorCharalampopoulos, I.en
dc.contributor.authorZervou, M.en
dc.contributor.authorVergou, V.en
dc.contributor.authorKatsanou, E. S.en
dc.contributor.authorLazaridis, I.en
dc.contributor.authorAlexis, M. N.en
dc.contributor.authorGravanis, A.en
dc.date.accessioned2015-11-24T19:01:31Z
dc.date.available2015-11-24T19:01:31Z
dc.identifier.issn1520-4804-
dc.identifier.urihttps://olympias.lib.uoi.gr/jspui/handle/123456789/19701
dc.rightsDefault Licence-
dc.subjectAnimalsen
dc.subjectApoptosis/*drug effectsen
dc.subjectCell Line, Tumoren
dc.subjectCell Proliferation/drug effectsen
dc.subjectDehydroepiandrosterone/adverse effects/*analogs & derivatives/*chemicalen
dc.subjectsynthesis/pharmacologyen
dc.subjectEstrogen Receptor alpha/agonists/biosynthesisen
dc.subjectEstrogen Receptor beta/agonists/biosynthesisen
dc.subjectHumansen
dc.subjectModels, Molecularen
dc.subjectMolecular Conformationen
dc.subjectNeurons/cytology/drug effectsen
dc.subjectNeuroprotective Agents/adverse effects/*chemical synthesis/pharmacologyen
dc.subjectRatsen
dc.subjectStructure-Activity Relationshipen
dc.titleNovel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activityen
heal.abstractDHEA analogues with modifications at positions C3 or C17 were synthesized and evaluated for neuroprotective activity against the neural-crest-derived PC12 cell model of serum deprivation-induced apoptosis. The most potent compounds were the spiro-epoxy derivatives 17beta-spiro[5-androstene-17,2'-oxiran]-3beta-ol (20), (20S)-3beta,21-dihydroxy-17beta,20-epoxy-5-pregnene (23), and (20R)-3beta,21-dihydroxy-17alpha,20-epoxy-5-pregnene (27) with IC(50) values of 0.19 +/- 0.01, 99.0 +/- 4.6, and 6.4 +/- 0.3 nM, respectively. Analogues 20, 23, and 27, up to the micromolar range of concentrations, were unable to activate estrogen receptor alpha and beta (ERalpha and ERbeta) or to interfere with ER-dependent gene expression significantly. In addition, they were unable to stimulate the growth of Ishikawa, MCF-7, and LNCaP cells. Our results suggest that the spiro-epoxyneurosteroid derivatives 20, 23, and 27 may prove to be lead molecules for the synthesis of novel neuroprotective agents.en
heal.accesscampus-
heal.fullTextAvailabilityTRUE-
heal.identifier.primary10.1021/jm900468p-
heal.identifier.secondaryhttp://www.ncbi.nlm.nih.gov/pubmed/19845386-
heal.identifier.secondaryhttp://pubs.acs.org/doi/pdfplus/10.1021/jm900468p-
heal.journalNameJ Med Chemen
heal.journalTypepeer-reviewed-
heal.languageen-
heal.publicationDate2009-
heal.recordProviderΠανεπιστήμιο Ιωαννίνων. Σχολή Επιστημών Υγείας. Τμήμα Ιατρικήςel
heal.typejournalArticle-
heal.type.elΆρθρο Περιοδικούel
heal.type.enJournal articleen

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