Structure-activity relationships study at the 3 '-N position of paclitaxel. Part 2: Synthesis and biological evaluation of 3 '-N-thiourea- and 3 '-N-thiocarbamate-bearing paclitaxel analogues

Citation
M. Xue et al., Structure-activity relationships study at the 3 '-N position of paclitaxel. Part 2: Synthesis and biological evaluation of 3 '-N-thiourea- and 3 '-N-thiocarbamate-bearing paclitaxel analogues, BIOORG MED, 10(12), 2000, pp. 1327-1331
Citations number
23
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960-894X → ACNP
Volume
10
Issue
12
Year of publication
2000
Pages
1327 - 1331
Database
ISI
SICI code
0960-894X(20000619)10:12<1327:SRSAT3>2.0.ZU;2-3
Abstract
The syntheses and preliminary biological evaluation of 3'-N-thiocarbamate- and 3'-N'-thiourea-bearing paclitaxel analogues, 4a-f and 5a-e, are describ ed. 3'-N-thiocarbamates 4a-e were found to be more potent than paclitaxel i n both the tubulin polymerization assay and the in vitro cytotoxicity assay . Several derivatives of this class such as 4c, 4d, and 4e also exhibited s ome in vivo activity. (C) 2000 Elsevier Science Ltd. All rights reserved.