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Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
- Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues
- Woo S.; Kang D.-H.; Nam J.M.; Lee C.S.; Ha E.-M.; Lee E.-S.; Kwon Y.; Na Y.
- Ewha Authors
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- European Journal of Medicinal Chemistry
- European Journal of Medicinal Chemistry vol. 45, no. 9, pp. 4221 - 4228
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- 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.
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