Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5849
Title: From Taxuspine X to structurally simplified Taxanes with remarkable P-Glycoprotein inhibitory activity
Authors: Castagnolo, Daniele
Contemori, Lorenzo
Maccari, Giorgio
S. I., Avramova
Neri, Alessandro
Sgaragli, GIAN PIETRO
Botta, Maurizio 
Keywords: Taxanes; MDR reversing agents; P-glycoprotein; macrolactone
Issue Date: 2010
Project: None 
Journal: ACS MEDICINAL CHEMISTRY LETTERS
Abstract: 
Three simplified “non-natural” natural taxanes, related to taxuspine X, were synthetized and assayed as P-glycoprotein (P-gp) inhibitors. One of them (6) proved to be a very efficient P-gp inhibitor with an IC50 = 7.2 × 10−6 M. In addition, to rationalize biological data, a pharmacophoric model was built through a ligand-based approach. This model represents the first example of a pharmacophore, which describes interactions of taxanes with P-gp.
Description: 
22244
URI: http://hdl.handle.net/20.500.12779/5849
ISSN: 1948-5875
DOI: 10.1021/ml100118k
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