Effects of the hydrophobicity of taxoids on their interaction with tubulin

Authors
Guenard, D Thoret, S Dubois, J Adeline, MT Wang, Q Gueritte, F
Citation
D. Guenard et al., Effects of the hydrophobicity of taxoids on their interaction with tubulin, BIO MED CH, 8(1), 2000, pp. 145-156
Citations number
34
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
8
Issue
1
Year of publication
2000
Pages
145 - 156
Database
ISI
SICI code
0968-0896(200001)8:1<145:EOTHOT>2.0.ZU;2-3
Abstract
Modifications of the hydrophobic character at the 7 and 10 positions of the taxoids greatly modified the effect of these drugs on the tubulin-microtub ule system. The presence of an alkyl chain at these positions decreased the activity while their corresponding more polar analogues restored the activ ity of these molecules. It appears that the recognition of taxoids by tubul in depends on the location of the most important hydrophobic area. (C) 2000 Elsevier Science Ltd. All rights reserved.