3-(3-Butylamino-2-hydroxy-propoxy)-1-hydroxy-xanthen-9-one acts as a topoisomerase II alpha catalytic inhibitor with low DNA damage

Title
3-(3-Butylamino-2-hydroxy-propoxy)-1-hydroxy-xanthen-9-one acts as a topoisomerase II alpha catalytic inhibitor with low DNA damage
Author(s)
이응석박소은[박소은]장인혜[장인혜]전규연[전규연]이은영[이은영]나영화[나영화]권영주[권영주]
Keywords
EXPRESSION; CANCER; ANTICANCER; MECHANISM; PATHWAY; AGENTS; CELLS
Issue Date
201311
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.69, pp.139 - 145
Abstract
As 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.
URI
http://hdl.handle.net/YU.REPOSITORY/28466http://dx.doi.org/10.1016/j.ejmech.2013.07.048
ISSN
0223-5234
Appears in Collections:
약학대학 > 약학부 > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE