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  • Title: Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506.
    Author: Ohkubo M, Kojiri K, Kondo H, Tanaka S, Kawamoto H, Nishimura T, Nishimura I, Yoshinari T, Arakawa H, Suda H, Morishima H, Nishimura S.
    Journal: Bioorg Med Chem Lett; 1999 May 03; 9(9):1219-24. PubMed ID: 10340602.
    Abstract:
    6-N-Amino analogues of NB-506 [6-N-formylamino-12,13-dihydro-1,11-dihydroxy-13-(beta-D-glucopyranosyl) -5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione] (3b) were synthesized and tested with respect to topoisomerase inhibition, cytotoxicity and anticancer effects. Among them, a 1,3-dihydroxypropane analogue (J-109,404, 5t) showed more than ten times more potent anticancer activity in MKN-45 human stomach cancer cells implanted in mice than NB-506.
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