Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506
作者:Mitsuru Ohkubo、Katsuhisa Kojiri、Hisao Kondo、Seiichi Tanaka、Hiroshi Kawamoto、Teruyuki Nishimura、Ikuko Nishimura、Tomoko Yoshinari、Hiroharu Arakawa、Hiroyuki Suda、Hajime Morishima、Susumu Nishimura
DOI:10.1016/s0960-894x(99)00188-2
日期:1999.5
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, St) showed more than ten times more potent anticancer activity in MKN-45 human stomach cancer cells implanted in mice than NB-506. (C) 1999 Elsevier Science Ltd. All rights reserved.