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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 7
BKCSDE 32(7)
July 20, 2011

Title	Synthesis, Cytotoxicity and Topoisomerase II Inhibitory Activity of Benzonaphthofurandiones
Author	Hee-Kyung Rhee, Youngjoo Kwon, Hwa-Jin Chung, Sang Kook Lee, Hea-Young Park Choo*
Keywords	Benzonaphthofurandiones, Cytotoxicity, Topoisomerase II
Abstract	Benzonaphthofurandiones containing four coplanar fused aromatic rings were synthesized and evaluated for their cytotoxicity against five human cancer cell lines, and their inhibitory activity on topoisomerases. These benzonaphthofurandiones were prepared by condensation of 2,3-dichloronaphthoquinone and three aromatic diols with base catalysts in alcohol. The synthesized compounds were o-alkylated with six dialkylaminoalkyl halides. The hydroxy derivatives (8a-8g) exhibited relatively potent cytotoxicity among the prepared compounds. These compounds were evaluated as excellent inhibitors against topoisomerase II (topo II). Especially, the hydroxy analogue with branched methyl side chain (8e) showed high cytotoxicity against cancer cell lines and good inhibitory activity on topo II.
Page	2391 - 2396
Full Text	PDF

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