title: Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors.
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.
authors.affiliation: Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Université Paris-Saclay , 1 Avenue de la Terrasse, 91198, Gif-sur-Yvette Cedex, France.
authors.forename: Olga
authors.initials: O
authors.lastname: Gherbovet
authors.affiliation: Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Université Paris-Saclay , 1 Avenue de la Terrasse, 91198, Gif-sur-Yvette Cedex, France.
authors.forename: María Concepción
authors.initials: MC
authors.lastname: García Alvarez
authors.affiliation: Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Université Paris-Saclay , 1 Avenue de la Terrasse, 91198, Gif-sur-Yvette Cedex, France.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Bignon
authors.affiliation: Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Université Paris-Saclay , 1 Avenue de la Terrasse, 91198, Gif-sur-Yvette Cedex, France.
authors.forename: Fanny
authors.initials: F
authors.lastname: Roussi
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells; D015394:Molecular Structure; D020112:Rhodamine 123 / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014747:Vinblastine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D031053:Vinca / Q000737:chemistry*; D000077235:Vinorelbine
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D020112:Rhodamine 123; D014747:Vinblastine; D004317:Doxorubicin; D000077235:Vinorelbine