Synthesis and Biological Properties of Luotonin A Derivatives 


Vol. 29,  No. 10, pp. 1988-1992, Oct.  2008
10.5012/bkcs.2008.29.10.1988


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  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.

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  Cite this article

[IEEE Style]

A. F. M. M. Rahman, D. H. Kim, J. L. Liang, E. S. Lee, Y. Na, K. Y. Jun, Y. Kwon, Y. Jahng, "Synthesis and Biological Properties of Luotonin A Derivatives," Bulletin of the Korean Chemical Society, vol. 29, no. 10, pp. 1988-1992, 2008. DOI: 10.5012/bkcs.2008.29.10.1988.

[ACM Style]

A F M Motiur Rahman, Dong Hyeon Kim, Jing Lu Liang, Eung Seok Lee, Younghwa Na, Kyu Yeon Jun, Youngjoo Kwon, and Yurngdong Jahng. 2008. Synthesis and Biological Properties of Luotonin A Derivatives. Bulletin of the Korean Chemical Society, 29, 10, (2008), 1988-1992. DOI: 10.5012/bkcs.2008.29.10.1988.