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dc.creatorJuranić, Ivan
dc.creatorTošić, Ana V.
dc.creatorKolundžija, Branka
dc.creatorDrakulić, Branko
dc.date.accessioned2019-04-20T13:42:45Z
dc.date.available2019-04-20T13:42:45Z
dc.date.issued2014
dc.identifier.issn1381-1991
dc.identifier.urihttp://cer.ihtm.bg.ac.rs/handle/123456789/2670
dc.description.abstractAntiproliferative activity of twenty one Michael adducts of aroylacrylic acids and cyclic amines ( N -Me-piperazine, imidazole, 2-Me-imidazole, and indole) was tested toward five human tumor cell lines (HeLa, LS174, K562, FemX, MDA-MB-361) in vitro. Compounds exerted antiproliferative activity in the high to the single-digit micromolar concentrations, causing increase of the cell population fraction in S phase and apoptosis. N -Me-piperazine and imidazole derivatives of aroylacrylic acids substituted with bulky alkyl substituents (2,4-di- i -Pr-Ph-, 2,4,6-tri-Et-Ph-, or β -tetrahydronaphthyl-) showed the best potency, while indole adducts were proved as the inferior antiproliferative agents. Few compounds showed significant selectivity, tumor versus healthy cells, with selectivity index ∼60 for the most selective congener. An unbiased in silico distinction between more and less potent compounds was obtained from 3D QSAR models derived by alignment-independent GRIND-2 descriptors.sr
dc.language.isoensr
dc.publisherSpringersr
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172035/RS//sr
dc.rightsrestrictedAccesssr
dc.sourceMolecular Diversitysr
dc.subjectAntiproliferative activitysr
dc.subjectSelectivitysr
dc.subjectMichael adductssr
dc.subjectAroylacrylic acidssr
dc.subject3D QSARsr
dc.titleAntiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic aminessr
dc.typearticlesr
dc.rights.licenseARRsr
dcterms.abstractКолунджија, Бранка; Тошић, Aна В.; Јуранић, Иван О.; Дракулиц, Бранко;
dc.rights.holderSpringersr
dc.citation.volume18
dc.citation.issue3
dc.citation.spage577
dc.citation.epage592
dc.citation.rankM21
dc.identifier.pmid24874228
dc.identifier.doi10.1007/s11030-014-9528-4
dc.identifier.scopus2-s2.0-84903818978
dc.identifier.wos000338641700009
dc.type.versionpublishedVersionsr


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