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New benzoxanthone derivatives as topoisomerase inhibitors and DNA cross-linkers

Title
New benzoxanthone derivatives as topoisomerase inhibitors and DNA cross-linkers
Authors
Cho H.-J.Jung M.-J.Woo S.Kim J.Lee E.-S.Kwon Y.Na Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2010
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 18, no. 3, pp. 1010 - 1017
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
We synthesized 12 benzoxanthone derivatives classified as three different groups based on the tetracyclic ring shapes and evaluated their pharmacological activities to find potential anticancer agents. In the cytotoxicity test, most compounds showed effective cancer cell growth inhibition against the HT29 and DU145 cell lines. Among the compounds tested, compound 19 was the most effective in the cancer cell lines tested. Compound 9 showed dual inhibitory activities against DNA relaxation by topoisomerases I and II. The% inhibition of compound 9 on topoisomerase I was comparable to that of camptothecin. Compound 9 efficiently blocked topoisomerase II function by almost threefold than etoposide at 20 μM. Compound 19 had selective topoisomerase II inhibitory activity at 100 μM. The DNA cross-linking test revealed that only compounds 8 and 19, which possess epoxy groups, cross-linked DNA duplex, while 14 did not. From the combined pharmacological results, we proposed that the target through which compound 19 inhibits cancer cell growth may be the DNA duplex itself and/or DNA-topoisomerase II complex. © 2010 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2009.12.069
Appears in Collections:
약학대학 > 약학과 > Journal papers
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