Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506

Authors
Ohkubo, M Kojiri, K Kondo, H Tanaka, S Kawamoto, H Nishimura, T Nishimura, I Yoshinari, T Arakawa, H Suda, H Morishima, H Nishimura, S
Citation
M. Ohkubo et al., Synthesis and biological activities of topoisomerase I inhibitors, 6-N-amino analogues of NB-506, BIOORG MED, 9(9), 1999, pp. 1219-1224
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
9
Year of publication
1999
Pages
1219 - 1224
Database
ISI
SICI code
0960-894X(19990503)9:9<1219:SABAOT>2.0.ZU;2-P
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 inh ibition, cytotoxicity and anticancer effects. Among them, a 1,3-dihydroxypr opane analogue (J-109,404, St) showed more than ten times more potent antic ancer activity in MKN-45 human stomach cancer cells implanted in mice than NB-506. (C) 1999 Elsevier Science Ltd. All rights reserved.