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Synthesis and Biological Properties of Luotonin a Derivatives

Title
Synthesis and Biological Properties of Luotonin a Derivatives
Authors
Rahman A.F.M.M.Dong H.K.Jing L.L.Lee E.-S.Na Y.Jun K.-Y.Kwon Y.Jahng Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2008
Journal Title
Bulletin of the Korean Chemical Society
ISSN
0253-2964JCR Link
Citation
vol. 29, no. 10, pp. 1988 - 1992
Indexed
SCI; SCIE; SCOPUS; KCI WOS scopus
Abstract
A series of new derivatives on the ring A of luotonin A were prepared by Friedländer 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.
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약학대학 > 약학과 > Journal papers
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