Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
- Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
- 우상욱[우상욱]; 강다혜[강다혜]; 남정민[남정민]; 이종순; 하은미[하은미]; 이응석; 권영주[권영주]; 나영화[나영화]
- DNA CROSS-LINKING; GAMMA-PYRONE COMPOUNDS; TOPOISOMERASE-II INHIBITION; POTENTIAL ANTICANCER DRUGS; XANTHONE DERIVATIVES; PSOROSPERMIN; CYTOTOXICITY; AGENTS
- Issue Date
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.45, no.9, pp.4221 - 4228
- 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.
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