Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues

Title
Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
Author(s)
우상욱[우상욱]강다혜[강다혜]남정민[남정민]이종순하은미[하은미]이응석권영주[권영주]나영화[나영화]
Keywords
DNA CROSS-LINKING; GAMMA-PYRONE COMPOUNDS; TOPOISOMERASE-II INHIBITION; POTENTIAL ANTICANCER DRUGS; XANTHONE DERIVATIVES; PSOROSPERMIN; CYTOTOXICITY; AGENTS
Issue Date
201009
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.45, no.9, pp.4221 - 4228
Abstract
In order to develop potential anti-cancer agents that act on topoisomerase II and DNA, we have synthesized 12 new xanthone derivatives. In the cytotoxicity test, compounds 17 and 31 exhibited 2- to 7-fold stronger inhibitory activity than adriamycin against most cancer cell lines tested. Halohydrin group-tethered compounds 19, 21 and 27 showed comparable topoisomerase II inhibitory activity to etoposide at 100 mu M concentration. In the DNA cross-linking test, compounds 20, 30 and 31 produced DNA cross-linked adducts and compound 30 was the strongest DNA cross-linker. Based on the combined pharmacological results, we suspected that the strong anti-cancer activity of compounds 16, 17, 20, 30 and 31 originated from the DNA mono-alkylation or cross-linking properties of the compounds. (C) 2010 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/23682http://dx.doi.org/10.1016/j.ejmech.2010.06.017
ISSN
0223-5234
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이과대학 > 화학생화학부 > Articles
약학대학 > 약학부 > Articles
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