Design, synthesis and antiproliferative activity of tripentones: A new series of antitubulin agents

Authors
Lisowski, V Enguehard, C Lancelot, JC Caignard, DH Lambel, S Leonce, S Pierre, A Atassi, G Renard, P Rault, S
Citation
V. Lisowski et al., Design, synthesis and antiproliferative activity of tripentones: A new series of antitubulin agents, BIOORG MED, 11(16), 2001, pp. 2205-2208
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
16
Year of publication
2001
Pages
2205 - 2208
Database
ISI
SICI code
0960-894X(20010820)11:16<2205:DSAAAO>2.0.ZU;2-#
Abstract
Structure-activity relationship studies of a new series of tripentones (thi eno[2.3-h]pyrrolizin-8-ones), led us to prepare several derivatives with an tiproliferative activities. The most promising 3-(3-hydroxy-4-methoxyphenyl )thieno[2.3-b]pyrrolizin-8-one 20 (leukemia L1210. IC50= 15 nM) was shown t o be a potent inhibitor of tubulin polymerization. (C) 2001 Elsevier Scienc e Ltd. All rights reserved.