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.

journal_name

J Med Chem

authors

Gherbovet O,García Alvarez MC,Bignon J,Roussi F

doi

10.1021/acs.jmedchem.6b00525

subject

Has Abstract

pub_date

2016-12-08 00:00:00

pages

10774-10780

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

59

pub_type

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