New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead

Authors
Wipf, P Hopkins, TD Jung, JK Rodriguez, S Birmingham, A Southwick, EC Lazo, JS Powis, G
Citation
P. Wipf et al., New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead, BIOORG MED, 11(19), 2001, pp. 2637-2641
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
19
Year of publication
2001
Pages
2637 - 2641
Database
ISI
SICI code
0960-894X(20011008)11:19<2637:NIOTTR>2.0.ZU;2-8
Abstract
Natural products of the naphthoquinone spiroketal structural type served as lead structures for the development of novel inhibitors of the thioredoxin -thioredoxin reductase redox. system. The most potent compound in this seri es inhibited thioredoxin with an IC50 of 350 nM, and many derivatives showe d low micromolar activities for growth inhibition against two breast cancer cell lines. (C) 2001 Elsevier Science Ltd. All rights reserved.