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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 10
BKCSDE 29(10)
October 20, 2008

Title	Synthesis and Biological Properties of Luotonin A Derivatives
Author	A F M Motiur Rahman, Dong Hyeon Kim, Jing Lu Liang, Eung Seok Lee, Younghwa Na, Kyu Yeon Jun, Youngjoo Kwon, Yurngdong Jahng
Keywords	Luotonin A, Topoisomerase I, Topoisomerase II, Cytotoxicity, Friedlander reaction
Abstract	A series of new derivatives on the ring A of luotonin A were prepared by Friedlander condensation of 6,7,8,10- tetrahydropyrrolo[2,1-b]quinazoline-6,10-dione and suitably substituted 2-aminobenzaldehydes and 2- aminoacetophenones. Their inhibitory activities on topoisomerases and cytotoxicities against selected human cancer cell lines were evaluated. Among the compounds tested, 8-fluoroluotonin A showed similar inhibitory activity on topoisomerase I comparable to camptothecin while luotonin A and 9-hydroxyluotonin A showed 1.37 and 0.94 times stronger inhibitory activity, respectively, on topoisomerase II compared to etoposide. Some derivatives of luotonin A showed moderate cytotoxicity. The possible relationship between the inhibitory activity on Topo II and the cytotoxicity of luotonin A and its analogues, thus, cannot be ruled out.
Page	1988 - 1992
Full Text	PDF

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