Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 권영주 | * |
dc.date.accessioned | 2016-08-27T04:08:03Z | - |
dc.date.available | 2016-08-27T04:08:03Z | - |
dc.date.issued | 2014 | * |
dc.identifier.issn | 0022-2623 | * |
dc.identifier.issn | 1520-4804 | * |
dc.identifier.other | OAK-12140 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/216948 | - |
dc.description.abstract | Fluorescein 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.language | English | * |
dc.publisher | AMER CHEMICAL SOC | * |
dc.title | Fluorescein Hydrazones as Novel Nonintercalative Topoisomerase Catalytic Inhibitors with Low DNA Toxicity | * |
dc.type | Article | * |
dc.relation.issue | 21 | * |
dc.relation.volume | 57 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 9139 | * |
dc.relation.lastpage | 9151 | * |
dc.relation.journaltitle | JOURNAL OF MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1021/jm501263m | * |
dc.identifier.wosid | WOS:000344977400033 | * |
dc.identifier.scopusid | 2-s2.0-84923782339 | * |
dc.author.google | Rahman, A. F. M. Motiur | * |
dc.author.google | Park, So-Eun | * |
dc.author.google | Kadi, Adnan A. | * |
dc.author.google | Kwon, Youngjoo | * |
dc.contributor.scopusid | 권영주(12446435600) | * |
dc.date.modifydate | 20240123101932 | * |