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dc.contributor.author김춘미*
dc.contributor.author김화정*
dc.contributor.author이상국*
dc.contributor.author서은경*
dc.date.accessioned2016-08-28T11:08:29Z-
dc.date.available2016-08-28T11:08:29Z-
dc.date.issued2003*
dc.identifier.issn0916-8451*
dc.identifier.otherOAK-1665*
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/219311-
dc.description.abstractA 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.languageEnglish*
dc.titleCytotoxicity and DNA topoisomerase inhibitory activity of benz[f]indole-4,9-dione analogs*
dc.typeArticle*
dc.relation.issue9*
dc.relation.volume67*
dc.relation.indexSCI*
dc.relation.indexSCIE*
dc.relation.indexSCOPUS*
dc.relation.startpage1944*
dc.relation.lastpage1949*
dc.relation.journaltitleBioscience, Biotechnology and Biochemistry*
dc.identifier.doi10.1271/bbb.67.1944*
dc.identifier.wosidWOS:000185727700014*
dc.identifier.scopusid2-s2.0-2842599309*
dc.author.googlePark H.J.*
dc.author.googleLee H.-J.*
dc.author.googleLee E.-J.*
dc.author.googleHwang H.J.*
dc.author.googleShin S.-H.*
dc.author.googleSuh M.-E.*
dc.author.googleKim C.*
dc.author.googleKim H.J.*
dc.author.googleSeo E.-K.*
dc.author.googleLee S.K.*
dc.contributor.scopusid김춘미(7409876240)*
dc.contributor.scopusid김화정(56670336100)*
dc.contributor.scopusid이상국(36067620500)*
dc.contributor.scopusid서은경(7005953758)*
dc.date.modifydate20240118124308*
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약학대학 > 약학과 > Journal papers
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