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Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors by Hee-Ju Cho; Mi-Ja Jung; Youngjoo Kwon; Younghwa Na is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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A total of seven new oxyranylmethyloxy or thiiranylmethyloxy group substituted 5-azaxanthones and -acridones analogues were synthesized and tested for their biological activities for cancer cell lines and topoisomerases. Among the compounds, compound 5, 3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone, showed effective topoisomerase I inhibitory activity, 50% and 27% inhibition ratio at 100 and 20 lM, respectively. This result is the first finding of the function of 5-azaxanthone compounds for topoisomerase I inhibition and can provide a novel skeleton for the anticancer drug development process.

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Author

Hee-Ju Cho; Mi-Ja Jung; Youngjoo Kwon; Younghwa Na

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)