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dc.creatorGaši, K.M.P.
dc.creatorBrenesel, M.Dj.D.
dc.creatorDjurendić, E.A.
dc.creatorSakač, Marija
dc.creatorČanadi, J.J.
dc.creatorDaljev, J.J.
dc.creatorArmbruster, T.
dc.creatorAndrić, Silvana
dc.creatorSladić, Dušan
dc.creatorBožić, Tatjana T.
dc.creatorNovaković, Irena
dc.creatorJuranić, Zorica
dc.date.accessioned2019-01-30T17:16:41Z
dc.date.available2019-01-30T17:16:41Z
dc.date.issued2007
dc.identifier.issn0039-128X
dc.identifier.urihttps://cer.ihtm.bg.ac.rs/handle/123456789/366
dc.description.abstractStarting from dehydroepiandrosterone (1) 17-picolyl (2), 17-picolinylidene (7), 17-picolinylidene-16-one (10 and 11), and 17-picolyl-16-one (15) derivatives of androst-5-ene were synthesized in one, two, four and five steps respectively. By the Oppenauer oxidation or dehydration of 2, 7, 10, and 11 with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), the corresponding A and B ring modified derivatives 3, 5, 6, 8, 9, and 12-14 were obtained. The structure of 2 was unambiguously proved by the appropriate X-ray structural analysis. Compounds 3, 5, 9, 12-14 showed inhibitory activity against the enzyme aromatase. Antibacterial activity, toxicity to brine shrimp Artemia salina, antitumor activity against three tumor cell lines (human cervix carcinoma HeLa cells, human melanoma FemX cells, and human myelogenous leukemia K562 cells) and toxicity against peripheral blood mononuclear cells were evaluated. Three tested compounds, namely 11, 13, and 15, showed strong activity against all three cell lines, the IC50 values being in the range of 4-10 μM.en
dc.publisherElsevier Science Inc, New York
dc.relationinfo:eu-repo/grantAgreement/MESTD/MPN2006-2010/142052/RS//
dc.rightsrestrictedAccess
dc.sourceSteroids
dc.subjectAndrost-5-ene derivativesen
dc.subjectAntibacterial activityen
dc.subjectAntitumor activityen
dc.subjectAromatase inhibitionen
dc.subjectPicolyl and picolinylidene derivativesen
dc.subjectX-ray analysisen
dc.titleSynthesis and biological evaluation of some 17-picolyl and 17-picolinylidene androst-5-ene derivativesen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractДаљев, Ј.Ј.; Сладић, Д.М.; Aрмбрустер, Т.; Бренесел, М.Дј.Д.; Дјурендић, Е.A.; Сакач, М.Н.; Aндрић, С.; Чанади, Ј.Ј.; Божић, Т.Т.; Новаковић, Ирена; Јуранић, З.Д.; Гаши, К.М.П.;
dc.citation.volume72
dc.citation.issue1
dc.citation.spage31
dc.citation.epage40
dc.citation.other72(1): 31-40
dc.citation.rankM22
dc.identifier.pmid17118415
dc.identifier.doi10.1016/j.steroids.2006.10.002
dc.identifier.rcubConv_4061
dc.identifier.scopus2-s2.0-33846020540
dc.identifier.wos000243861100004
dc.type.versionpublishedVersion


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