From taxuspine X to structurally simplified taxanes with remarkable P-Glycoprotein inhibitory activity

Castagnolo, Daniele, Contemori, Lorenzo, Maccari, Giorgio, Avramova, Stanislava, Neri, Annalisa, Sgaragli, Gianpietro and Botta, Maurizio (2010) From taxuspine X to structurally simplified taxanes with remarkable P-Glycoprotein inhibitory activity. ACS Medicinal Chemistry Letters, 1 (8). pp. 416-421. ISSN 1948-5875

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Official URL: http://dx.doi.org/10.1021/ml100118k

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.

Item Type: Article
Uncontrolled Keywords: taxanes, MDR reversing agents, P-glycoprotein, macrolactone, non-natural natural product
Subjects: F100 Chemistry
Department: Faculties > Health and Life Sciences > School of Life Sciences > Applied Sciences
Depositing User: Linda Barlow
Date Deposited: 09 Jan 2013 10:15
Last Modified: 10 Aug 2015 11:42
URI: http://nrl.northumbria.ac.uk/id/eprint/10977

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