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dc.contributor.author권영주-
dc.date.accessioned2016-08-27T04:08:03Z-
dc.date.available2016-08-27T04:08:03Z-
dc.date.issued2014-
dc.identifier.issn0022-2623-
dc.identifier.issn1520-4804-
dc.identifier.otherOAK-12140-
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/216948-
dc.description.abstractFluorescein hydrazones (3a-3l) were synthesized in three steps with 86-91% overall yields. Topo I- and IIa-mediated relaxation and cell viability assay were evaluated. 3d inhibited 47% Topo I (camptothecin, 34%) and 20% Topo II (etoposide 24%) at 20 mu M. 3l inhibited 61% Topo II (etoposide 24%) at 20 mu M. 3d and 3l were further evaluated to determine their mode of action with diverse methods of kDNA decatenation, DNA-Topo cleavage complex, comet, DNA intercalating/unwinding, and Topo IIa-mediated ATP hydrolysis assays. 3d functioned as a nonintercalative dual inhibitor against the catalytic activities of Topo I and Topo II alpha. 3l acted as a Topo IIa specific nonintercalative catalytic inhibitor. 3d activated apoptotic proteins as it increased the level of cleaved capase-3 and cleaved PARP in a dose- and time-dependent manner. The dose- and time-dependent increase of G1 phase population was observed by treatment of 3d along with the increase of p27(kip1) and the decrease of cyclin D1 expression.-
dc.languageEnglish-
dc.publisherAMER CHEMICAL SOC-
dc.titleFluorescein Hydrazones as Novel Nonintercalative Topoisomerase Catalytic Inhibitors with Low DNA Toxicity-
dc.typeArticle-
dc.relation.issue21-
dc.relation.volume57-
dc.relation.indexSCI-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.startpage9139-
dc.relation.lastpage9151-
dc.relation.journaltitleJOURNAL OF MEDICINAL CHEMISTRY-
dc.identifier.doi10.1021/jm501263m-
dc.identifier.wosidWOS:000344977400033-
dc.identifier.scopusid2-s2.0-84923782339-
dc.author.googleRahman, A. F. M. Motiur-
dc.author.googlePark, So-Eun-
dc.author.googleKadi, Adnan A.-
dc.author.googleKwon, Youngjoo-
dc.contributor.scopusid권영주(12446435600;57281846700)-
dc.date.modifydate20220119154509-
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약학대학 > 약학과 > Journal papers
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