Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김춘미 | * |
dc.contributor.author | 김화정 | * |
dc.contributor.author | 이상국 | * |
dc.contributor.author | 서은경 | * |
dc.date.accessioned | 2016-08-28T11:08:29Z | - |
dc.date.available | 2016-08-28T11:08:29Z | - |
dc.date.issued | 2003 | * |
dc.identifier.issn | 0916-8451 | * |
dc.identifier.other | OAK-1665 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/219311 | - |
dc.description.abstract | A series of benz[f]indole-4,9-diones, based on the antitumor activity of 1,4-naphthoquinone, were synthesized and evaluated for their cytotoxic activity in cultured human cancer cell lines A549 (lung cancer), Col2 (colon cancer), and SNU-638 (stomach cancer), and also for the inhibition of human DNA topoisomerases I and II activity in vitro. Several compounds including 2-amino-3-ethoxycarbonyl-N-methyl-benz[f]indole-4,9-dione showed a potential cytotoxic activity judged by IC 50 < 20.0 μg/ml in the panel of cancer cell lines. Especially, 2-hydroxy-3-ethoxycarbonyl-N-(3,4-dimethylphenyl) -benz[f]indole-4,9-dione had potential selective cytotoxicity against lung cancer cells (IC 50= 0.4 μg/ml)) compared to colon (IC 50 > 20.0 μg/ml) and stomach (IC 50 > 20.0 μg/ml) cancer cells. To further investigate the cytotoxic mechanism, the effects of test compounds on DNA topoisomerase I and II activities were used. In a topoisomerase I-mediated relaxation assay using human placenta DNA topoisomerase I and supercoiled pHOTI plasmid DNA, 2-amino-3-ethoxycarbonyl-N-(4-fluorophenyl)- benz[f]indole-4,9-dione had the most potent inhibitory activity among the compounds tested. However, most of the compounds showed only weak inhibition of the DNA topoisomerase II-mediated KDNA (Kinetoplast DNA) decatenation assay, except for 2-amino-3-ethoxycarbonyl-N-(4-methylphenyl)-benz[f]indole-4,9-dione and 2-amino-3-ethoxycarbonyl-N-(2-bromoehtyl)-benz[f]indole-4,9-dione with a moderate inhibitory activity. These results suggest that several active compounds had relatively selective inhibitory activity against toposiomearse I compared to toposiomerase II. No obvious correlation was observed between the cytotoxicity of the individual compound and the inhibitory activity of DNA relaxation and decatenation by topoisomerase I and II, respectively, in vitro. | * |
dc.language | English | * |
dc.title | Cytotoxicity and DNA topoisomerase inhibitory activity of benz[f]indole-4,9-dione analogs | * |
dc.type | Article | * |
dc.relation.issue | 9 | * |
dc.relation.volume | 67 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 1944 | * |
dc.relation.lastpage | 1949 | * |
dc.relation.journaltitle | Bioscience, Biotechnology and Biochemistry | * |
dc.identifier.doi | 10.1271/bbb.67.1944 | * |
dc.identifier.wosid | WOS:000185727700014 | * |
dc.identifier.scopusid | 2-s2.0-2842599309 | * |
dc.author.google | Park H.J. | * |
dc.author.google | Lee H.-J. | * |
dc.author.google | Lee E.-J. | * |
dc.author.google | Hwang H.J. | * |
dc.author.google | Shin S.-H. | * |
dc.author.google | Suh M.-E. | * |
dc.author.google | Kim C. | * |
dc.author.google | Kim H.J. | * |
dc.author.google | Seo E.-K. | * |
dc.author.google | Lee S.K. | * |
dc.contributor.scopusid | 김춘미(7409876240) | * |
dc.contributor.scopusid | 김화정(56670336100) | * |
dc.contributor.scopusid | 이상국(36067620500) | * |
dc.contributor.scopusid | 서은경(7005953758) | * |
dc.date.modifydate | 20240118124308 | * |