dc.date.accessioned | 2021-04-23T19:32:03Z | |
dc.date.available | 2022-10-23T22:45:53Z | |
dc.date.created | 2021-02-19T15:35:48Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Xu, Chenhao Zhou, Wenjuan Dong, Guanjun Qiao, Hui Peng, Jiadi Jia, Pengfei Li, Yuhao Liu, Hongmin Sun, Kai Zhao, Wen . Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing hydrazone fragment as potent and selective anticancer agents. Bioorganic chemistry (Print). 2020, 105:104424, 1-16 | |
dc.identifier.uri | http://hdl.handle.net/10852/85505 | |
dc.description.abstract | In this paper, based on molecular hybridization, a series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing hydrazine was synthesized and their antiproliferative activities against 5 cancer cell lines (MGC-803, PC3, PC9, EC9706 and SMMC-7721) were evaluated. We found that most of them exhibited obvious growth inhibition effects on these tested cancer cells, especially compound 34 on PC3 cells (IC50 = 26.25 ± 0.28 nM). Meanwhile, compound 34 displayed best selectivity on PC3, compared with the other cancer cell lines, as well as excellent selectivity towards normal cell lines (Het-1A, L02 and GES-1). Further investigations demonstrated that 34 could significantly inhibit PC3 cells’ colony formation, increase cellular ROS content, suppress EGFR expression and induce apoptosis. Our findings indicate that 34 may serve as a novel lead compound for the discovery of more triazolopyrimidine derivatives with improved anticancer potency and selectivity. | |
dc.language | EN | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 International | |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | |
dc.title | Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing hydrazone fragment as potent and selective anticancer agents | |
dc.type | Journal article | |
dc.creator.author | Xu, Chenhao | |
dc.creator.author | Zhou, Wenjuan | |
dc.creator.author | Dong, Guanjun | |
dc.creator.author | Qiao, Hui | |
dc.creator.author | Peng, Jiadi | |
dc.creator.author | Jia, Pengfei | |
dc.creator.author | Li, Yuhao | |
dc.creator.author | Liu, Hongmin | |
dc.creator.author | Sun, Kai | |
dc.creator.author | Zhao, Wen | |
cristin.unitcode | 185,53,18,13 | |
cristin.unitname | Avdeling for patologi | |
cristin.ispublished | true | |
cristin.fulltext | postprint | |
cristin.qualitycode | 1 | |
dc.identifier.cristin | 1891866 | |
dc.identifier.bibliographiccitation | info:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioorganic chemistry (Print)&rft.volume=105:104424&rft.spage=1&rft.date=2020 | |
dc.identifier.jtitle | Bioorganic chemistry (Print) | |
dc.identifier.volume | 105 | |
dc.identifier.doi | https://doi.org/10.1016/j.bioorg.2020.104424 | |
dc.identifier.urn | URN:NBN:no-88190 | |
dc.type.document | Tidsskriftartikkel | |
dc.type.peerreviewed | Peer reviewed | |
dc.source.issn | 0045-2068 | |
dc.identifier.fulltext | Fulltext https://www.duo.uio.no/bitstream/handle/10852/85505/2/Postnr%2B1891866_Xu%2Bet%2Bal_Bioorg%2BChem%2B2020.pdf | |
dc.type.version | AcceptedVersion | |
cristin.articleid | 104424 | |