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ID: ALA3860099
Journal: J Med Chem
Title: Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
Authors: Gherbovet O, García Alvarez MC, Bignon J, Roussi F.
Abstract: The first example of vinca derivatives 16-18 able to modulate P-glycoprotein (Pgp) efflux activity is reported. They were elaborated in two steps from vinorelbine 3 (VLN) by a modification of the velbenamine moiety. These compounds were able to decrease efficiently Pgp mediated influx and efflux of rhodamine-123 (Rho) and to restore the cytotoxicity of vinorelbine 3 (VLN) and doxorubicin (Dox) on K562R (dox-resistant) cell lines.
CiteXplore: 27753480