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Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues

Title
Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
Authors
Woo S.Kang D.-H.Nam J.M.Lee C.S.Ha E.-M.Lee E.-S.Kwon Y.Na Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2010
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 45, no. 9, pp. 4221 - 4228
Indexed
SCI; SCIE; SCOPUS WOS scopus
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 μM 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. In order to develop potential anti-cancer agents that act on topoisomerase II and DNA, we have synthesized 12 new xanthone derivatives. © 2010 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2010.06.017
Appears in Collections:
약학대학 > 약학과 > Journal papers
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