Naphthazarin derivatives (II): Formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity

Authors
Song, GY Zheng, XG Kim, Y You, YJ Sok, DE Ahn, BZ
Citation
Gy. Song et al., Naphthazarin derivatives (II): Formation of glutathione conjugate, inhibition of DNA topoisomerase-I and cytotoxicity, BIOORG MED, 9(16), 1999, pp. 2407-2412
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
16
Year of publication
1999
Pages
2407 - 2412
Database
ISI
SICI code
0960-894X(19990816)9:16<2407:ND(FOG>2.0.ZU;2-J
Abstract
6-(1-Hydroxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones, expressing a higher r eactivity in conjugation with glutathione, showed a greater potency in the inhibition of DNA topoisomerase-I and the cytotoxicity against L1210 cells than 2-(1-hydroxyalkyl)-DMNQ derivatives, implying the participation of ele ctrophilic arylation in the bioactivities. In further study 6-(1-Hydroxyalk yl)-5,8-dimethoxy-1,4-naphthoquinones with an alkyl group of shorter chain length (C-2 similar to C-6) exerted a greater bioactivities than those with longer chain length(>C-6). (C) 1999 Elsevier Science Ltd. All rights reser ved.