Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors

Journal of Medicinal Chemistry
2016.0

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.

Knowledge Graph

Similar Paper

Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors
Journal of Medicinal Chemistry 2016.0
Vinflunine (20′,20′-difluoro- 3′,4′-dihydrovinorelbine), a novel Vinca alkaloid, which participates in P-glycoprotein (Pgp)-mediated multidrug resistance in vivo and in vitro
Investigational New Drugs 1998.0
Vinflunine (20′,20′-difluoro- 3′,4′-dihydrovinorelbine), a novel Vinca alkaloid, which participates in P-glycoprotein (Pgp)-mediated multidrug resistance in vivo and in vitro
Investigational New Drugs 1998.0
Vinblastine 20′ Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance
Journal of Medicinal Chemistry 2017.0
Arylmethyloxyphenyl Derivatives:  Small Molecules Displaying P-Glycoprotein Inhibition
Journal of Medicinal Chemistry 2006.0
Structure−activity relationship study of novel 2-aminobenzofuran derivatives as P-glycoprotein inhibitors
European Journal of Medicinal Chemistry 2017.0
Potent P-glycoprotein inhibition of emodin derivative: synthesis and biological evaluation
Medicinal Chemistry Research 2014.0
Flavonoid-Related Modulators of Multidrug Resistance:  Synthesis, Pharmacological Activity, and Structure−Activity Relationships
Journal of Medicinal Chemistry 1999.0
New triazine derivatives as potent modulators of multidrug resistance
Journal of Medicinal Chemistry 1992.0
Synthesis and structure–activity relationship studies of cytotoxic vinorelbine amide analogues
Bioorganic & Medicinal Chemistry Letters 2012.0