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

Daniele Castagnolo, Lorenzo Contemori, Giorgio Maccari, Stanislava Avramova, Annalisa Neri, Gianpietro Sgaragli, Maurizio Botta

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)416-421
JournalACS Medicinal Chemistry Letters
Volume1
Issue number8
DOIs
Publication statusPublished - 2010

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