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dc.creatorRupar, Jelena
dc.creatorDobričić, Vladimir
dc.creatorGrahovac, Jelena
dc.creatorRadulović, Siniša
dc.creatorSkok, Žiga
dc.creatorIlaš, Janez
dc.creatorAleksić, Mara
dc.creatorBrborić, Jasmina
dc.creatorČudina, Olivera
dc.date.accessioned2020-06-15T10:06:36Z
dc.date.available2020-06-15T10:06:36Z
dc.date.issued2020
dc.identifier.issn2632-8682
dc.identifier.urihttp://farfar.pharmacy.bg.ac.rs/handle/123456789/3606
dc.description.abstractA series of eleven 9-acridinyl amino acid derivatives were synthesized using a two-step procedure. Cytotoxicity was tested on the K562 and A549 cancer cell lines and normal diploid cell line MRC5 using the MTT assay. Compounds 6, 7, 8 and 9 were the most active, with IC50 values comparable to or lower than that of chemotherapeutic agent amsacrine. 8 and 9 were especially effective in the A549 cell line (IC50 ≈ 6 μM), which is of special interest since amsacrine is not sufficiently active in lung cancer patients. Cell cycle analysis revealed that 7 and 9 caused G2/M block, amsacrine caused arrest in the S phase, while 6 and 8 induced apoptotic cell death independently of the cell cycle regulation. In comparison to amsacrine, 6, 7, 8, and 9 showed similar inhibitory potential towards topoisomerase II, whereas only 7 showed DNA intercalation properties. In contrast to amsacrine, 6, 7, 8 and 9 showed a lack of toxicity towards unstimulated normal human leucocytes.en
dc.publisherRoyal Society of Chemistry
dc.relationinfo:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS//
dc.relationinfo:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41026/RS//
dc.rightsrestrictedAccess
dc.sourceRSC Medicinal Chemistry
dc.titleSynthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivativesen
dc.typearticle
dc.rights.licenseARR
dcterms.abstractСкок, Жига; Радуловић, Синиша; Рупар, Јелена; Добричић, Владимир; Aлексић, Мара; Брборић, Јасмина; Чудина, Оливера; Граховац, Јелена; Илаш, Јанез;
dc.citation.volume11
dc.citation.issue3
dc.citation.spage378
dc.citation.epage386
dc.identifier.wos000526953000005
dc.identifier.doi10.1039/c9md00597h
dc.identifier.doi2-s2.0-85083014447
dc.identifier.scopus2-s2.0-85083014447
dc.type.versionpublishedVersion


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