Jatrophane diterpenes as P-glycoprotein inhibitors. First insights of structure-activity relationships and discovery of a new, powerful lead

Gabriella Corea, Ernesto Fattorusso, Virginia Lanzotti, Orazio Taglialatela-Scafati, Giovanni Appendino, Mauro Ballero, Pierre Noël Simon, Charles Dumontet, Attilio Di Pietro

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

The Mediterranean spurge Euphorbia dendroides L. afforded a series of 10 closely related jatrophane polyesters, nine of which are new, which served as a base for the establishment of structure-activity relationships within this class of P-glycoprotein inhibitors. The results, while pointing to the general role of lipophilicity for activity, also highlighted the relevance of the substitution pattern at the positions 2, 3, and 5, suggesting the involvement of this fragment in binding. The most powerful compound of the series, euphodendroidin D (4), outperformed cyclosporin by a factor of 2 to inhibit Pgp-mediated daunomycin transport.

Lingua originaleInglese
pagine (da-a)3395-3402
Numero di pagine8
RivistaJournal of Medicinal Chemistry
Volume46
Numero di pubblicazione15
DOI
Stato di pubblicazionePubblicato - 17 lug 2003
Pubblicato esternamente

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