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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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 > Applied Sciences
Depositing User:	Linda Barlow
Date Deposited:	09 Jan 2013 10:15
Last Modified:	12 Oct 2019 18:26
URI:	http://nrl.northumbria.ac.uk/id/eprint/10977

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