dc.creator | Rupar, Jelena | |
dc.creator | Dobričić, Vladimir | |
dc.creator | Grahovac, Jelena | |
dc.creator | Radulović, Siniša | |
dc.creator | Skok, Žiga | |
dc.creator | Ilaš, Janez | |
dc.creator | Aleksić, Mara | |
dc.creator | Brborić, Jasmina | |
dc.creator | Čudina, Olivera | |
dc.date.accessioned | 2020-06-15T10:06:36Z | |
dc.date.available | 2020-06-15T10:06:36Z | |
dc.date.issued | 2020 | |
dc.identifier.issn | 2632-8682 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/3606 | |
dc.description.abstract | A 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.publisher | Royal Society of Chemistry | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172041/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Integrated and Interdisciplinary Research (IIR or III)/41026/RS// | |
dc.rights | restrictedAccess | |
dc.source | RSC Medicinal Chemistry | |
dc.title | Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Скок, Жига; Радуловић, Синиша; Рупар, Јелена; Добричић, Владимир; Aлексић, Мара; Брборић, Јасмина; Чудина, Оливера; Граховац, Јелена; Илаш, Јанез; | |
dc.citation.volume | 11 | |
dc.citation.issue | 3 | |
dc.citation.spage | 378 | |
dc.citation.epage | 386 | |
dc.citation.rank | M23 | |
dc.identifier.wos | 000526953000005 | |
dc.identifier.doi | 10.1039/c9md00597h | |
dc.identifier.doi | 2-s2.0-85083014447 | |
dc.identifier.scopus | 2-s2.0-85083014447 | |
dc.type.version | publishedVersion | |