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dc.contributor.author이응석ko
dc.contributor.author박소은[박소은]ko
dc.contributor.author장인혜[장인혜]ko
dc.contributor.author전규연[전규연]ko
dc.contributor.author이은영[이은영]ko
dc.contributor.author나영화[나영화]ko
dc.contributor.author권영주[권영주]ko
dc.date.accessioned2015-12-17T02:30:43Z-
dc.date.available2015-12-17T02:30:43Z-
dc.date.created2015-11-13-
dc.date.issued201311-
dc.identifier.citationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.69, pp.139 - 145-
dc.identifier.issn0223-5234-
dc.identifier.urihttp://hdl.handle.net/YU.REPOSITORY/28466-
dc.identifier.urihttp://dx.doi.org/10.1016/j.ejmech.2013.07.048-
dc.description.abstractAs a continuous study we prepared several alkylamine (n = 3-6) and evaluated for the pharmacological activity and mode of action. In the topoisomerase II alpha (topo II alpha) inhibition test, compound 4 showed strongest inhibitory activity among the compounds at 10 mu M. Inhibitory activities of the compounds are in the order of 4 (n = 4) > 1 (n = 3) >> 5 (n = 5) approximate to 6 (n = 6); 8 (n = 4) >> 7 (n = 3) approximate to 9(n = 5) approximate to 10 (n = 6) where n is the number of carbon in the aliphatic side chain in ring C and compounds 7-10 have additional methoxy group in ring A compared to compounds 1, 4-6. Compound 4 showed efficient cytotoxicities against T47D (IC50: 0.93 +/- 0.04 mu M) and HCT15 (IC50: 0.78 +/- 0.01 mu M) cells, which are higher than etoposide. Compound 4 was also an ATP-competitive human topo Hoc catalytic inhibitor with partially blocking human topo II alpha-catalyzed ATP hydrolysis and intercalating into DNA. Compound 4 induced much less DNA damage than etoposide in HCT15 human colorectal carcinoma cells. Overall, compound 4 can be a potential anticancer agent acting as topo II alpha catalytic inhibitor with low DNA damage. (C) 2013 Elsevier Masson SAS. All rights reserved.-
dc.language영어-
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER-
dc.subjectEXPRESSION-
dc.subjectCANCER-
dc.subjectANTICANCER-
dc.subjectMECHANISM-
dc.subjectPATHWAY-
dc.subjectAGENTS-
dc.subjectCELLS-
dc.title3-(3-Butylamino-2-hydroxy-propoxy)-1-hydroxy-xanthen-9-one acts as a topoisomerase II alpha catalytic inhibitor with low DNA damage-
dc.typeArticle-
dc.identifier.wosid000330603900013-
dc.identifier.scopusid2-s2.0-84883511339-
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