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.
| Original language | English |
|---|---|
| Pages (from-to) | 4221-4228 |
| Number of pages | 8 |
| Journal | European Journal of Medicinal Chemistry |
| Volume | 45 |
| Issue number | 9 |
| DOIs | |
| State | Published - Sep 2010 |
Bibliographical note
Funding Information:This work was supported by the Korea Research Foundation Grant funded by the Korean Government (MOEHRD) ( KRF-2006-521-E00159 ). J.M.N. was partially supported by the Brain Korea 21 project.
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- Anticancer activities
- DNA cross-linking
- Methyloxiranylmethoxyxanthones
- Oxiranylmethoxyxanthones
- Topoisomerase II inhibition
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