Synthesis and microtubule binding of fluorescent paclitaxel derivatives

Authors
Baloglu, E Kingston, DGI Patel, P Chatterjee, SK Bane, SL
Citation
E. Baloglu et al., Synthesis and microtubule binding of fluorescent paclitaxel derivatives, BIOORG MED, 11(17), 2001, pp. 2249-2252
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
17
Year of publication
2001
Pages
2249 - 2252
Database
ISI
SICI code
0960-894X(20010903)11:17<2249:SAMBOF>2.0.ZU;2-7
Abstract
The preparation of two new fluorescent derivatives of paclitaxel in which t he fluorophore is bonded to paclitaxel at the C-10 position is reported, Bo th analogues, 10-deacetyl-10-(m-aminobenzoyl)paclitaxel (1, BTax) and 10-dc acetyl-10-[7-(diethylamino) coumarin-3-carbonyl]paclitaxel (2, CTax) retain good activity as promoters of in vitro tubulin assembly. Microtubule bindi ng enhances the emission intensity of both probes. (C) 2001 Elsevier Scienc e Ltd. All rights reserved.