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dc.creatorVujatović, Tamara B.
dc.creatorVitorović - Todorović, Maja D.
dc.creatorCvijetić, Ilija
dc.creatorVasović, Tamara
dc.creatorNikolić, Milan R.
dc.creatorNovaković, Irena
dc.creatorBjelogrlić, Snežana
dc.date.accessioned2021-11-22T10:00:09Z
dc.date.available2021-11-22T10:00:09Z
dc.date.issued2022
dc.identifier.issn0022-2860
dc.identifier.urihttps://cer.ihtm.bg.ac.rs/handle/123456789/4853
dc.description.abstractIn the present work, the α, β-double bond of the aroylacrylic acid phenylamides was suitably modified to optimize the toxicity–antiproliferative activity ratio of the resulting compounds 1 –5 . The phenylamides were modified by Michael’s addition of suitably chosen piperidine-containing fragments: 1-amino-N- benzylpiperidine ( a1 ), 4-benzylpiperidine ( a2 ), and N , N -dimethyl- N -[2-(1-piperazinyl)-ethyl]amine ( a3 ). The compounds exerted micromolar activity toward three cancer cell lines, A549, LoVo, and Skov-3, caus- ing apoptotic cell death. It was shown that the nature of the cyclic amine moiety at position C2 of the compounds is probably the primary determinant of anticancer activity toward tested cell lines and the acute toxicity toward brine shrimp ( Artemia salina ). The majority of compounds revealed the ability to vigorously induce mitochondrial superoxide anion generation in all treated cell lines, which together with cell cycle arrest at the S phase and activation of intrinsic caspase cascade, indicates the possibility that apoptosis was triggered due to irreparable chromosomal damage by acute oxidative stress. Two deriva- tives also exerted significant antibacterial activity with one order of magnitude higher potency than chlo- ramphenicol in most of the investigated bacterial strains. Also, the drug-like properties for all compounds were estimated by available software tools.sr
dc.language.isoensr
dc.publisherElseviersr
dc.relationinfo:eu-repo/grantAgreement/MESTD/inst-2020/200325/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/inst-2020/200168/RS//sr
dc.relationinfo:eu-repo/grantAgreement/MESTD/inst-2020/200026/RS//sr
dc.relation.isversionofhttps://cer.ihtm.bg.ac.rs/handle/123456789/4857
dc.rightsrestrictedAccesssr
dc.sourceJournal of Molecular Structuresr
dc.subjectphenylamidessr
dc.subjectcancersr
dc.subjecttoxicitysr
dc.subjectdrug-like propertiessr
dc.titleNovel derivatives of aroylacrylic acid phenylamides as inducers of apoptosis through the ROS-mediated pathway in several cancer cell linessr
dc.typearticlesr
dc.rights.licenseARRsr
dc.citation.volume1250
dc.citation.spage131702
dc.citation.rankM22~
dc.description.otherThe peer-reviewed version: [https://cer.ihtm.bg.ac.rs/handle/123456789/4857]
dc.identifier.doi10.1016/j.molstruc.2021.131702
dc.identifier.scopus2-s2.0-85117959646
dc.identifier.wos000718042800003
dc.type.versionpublishedVersionsr


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