NOVEL LIGNAN DERIVATIVES AS SELECTIVE INHIBITORS OF DNA TOPOISOMERASE-II

Authors
KASHIWADA Y BASTOW KF LEE KH
Citation
Y. Kashiwada et al., NOVEL LIGNAN DERIVATIVES AS SELECTIVE INHIBITORS OF DNA TOPOISOMERASE-II, Bioorganic & medicinal chemistry letters, 5(8), 1995, pp. 905-908
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
8
Year of publication
1995
Pages
905 - 908
Database
ISI
SICI code
0960-894X(1995)5:8<905:NLDASI>2.0.ZU;2-R
Abstract
Rabdosiin (1) and its isomer (2), isolated from Arnebia euchroma, were potent non-selective inhibitors of mammalian DNA topoisomerases in vi tro. Evaluation of synthetic analogs led to the discovery of 3 - 5 as selective inhibitors of topoisomerase II. Unlike etoposide, which inhi bits by preventing the DNA rejoining process, compounds 1 - 5 did not induce DNA breakage in either cellular or in vine assay systems.