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Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines
dc.creator | Juranić, Ivan | |
dc.creator | Tošić, Ana V. | |
dc.creator | Kolundžija, Branka | |
dc.creator | Drakulić, Branko | |
dc.date.accessioned | 2019-04-20T13:42:45Z | |
dc.date.available | 2019-04-20T13:42:45Z | |
dc.date.issued | 2014 | |
dc.identifier.issn | 1381-1991 | |
dc.identifier.uri | https://cer.ihtm.bg.ac.rs/handle/123456789/2670 | |
dc.description.abstract | Antiproliferative 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. | en |
dc.language.iso | en | sr |
dc.publisher | Springer | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172035/RS// | sr |
dc.rights | restrictedAccess | sr |
dc.source | Molecular Diversity | sr |
dc.subject | Antiproliferative activity | sr |
dc.subject | Selectivity | sr |
dc.subject | Michael adducts | sr |
dc.subject | Aroylacrylic acids | sr |
dc.subject | 3D QSAR | sr |
dc.title | Antiproliferative activity of the Michael adducts of aroylacrylic acids and cyclic amines | en |
dc.type | article | sr |
dc.rights.license | ARR | sr |
dcterms.abstract | Колунджија, Бранка; Тошић, Aна В.; Јуранић, Иван О.; Дракулиц, Бранко; | |
dc.rights.holder | Springer | sr |
dc.citation.volume | 18 | |
dc.citation.issue | 3 | |
dc.citation.spage | 577 | |
dc.citation.epage | 592 | |
dc.citation.rank | M21 | |
dc.identifier.pmid | 24874228 | |
dc.identifier.doi | 10.1007/s11030-014-9528-4 | |
dc.identifier.scopus | 2-s2.0-84903818978 | |
dc.identifier.wos | 000338641700009 | |
dc.type.version | publishedVersion | sr |