Development of small-molecule P-gp inhibitors of the N-benzyl 1,4-dihydropyridine type: Novel aspects in SAR and bioanalytical evaluation of multidrug resistance (MDR) reversal properties

Bioorganic & Medicinal Chemistry
2013.0

Abstract

Novel series of N-benzyl 1,4-dihydropyridines have been prepared by facile syntheses. All relevant substituents of the molecular scaffold have been varied. The resulting compounds were biologically evaluated as P-glycoprotein (P-gp) inhibitors. Substitutions of the N-benzyl residue favour biological activity beside respective 3-ester functions. Most active compounds were further evaluated as multidrug resistance (MDR) modulators to restore the cytotoxic properties of varying daunorubicin applications.

Knowledge Graph

Similar Paper

Development of small-molecule P-gp inhibitors of the N-benzyl 1,4-dihydropyridine type: Novel aspects in SAR and bioanalytical evaluation of multidrug resistance (MDR) reversal properties
Bioorganic & Medicinal Chemistry 2013.0
Biological Evaluation of Bishydroxymethyl-Substituted Cage Dimeric 1,4-Dihydropyridines as a Novel Class of P-Glycoprotein Modulating Agents in Cancer Cells
Journal of Medicinal Chemistry 2006.0
Structure–activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors
Bioorganic & Medicinal Chemistry 2007.0
Novel structure–activity relationships and selectivity profiling of cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators
Bioorganic & Medicinal Chemistry 2010.0
Design and synthesis of new potent N,N -bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents
European Journal of Medicinal Chemistry 2018.0
1-[3-(2-Hydroxyethylsulfanyl)propanoyl]-3,5-bis(benzylidene)-4-piperidones: A novel cluster of P-glycoprotein dependent multidrug resistance modulators
Bioorganic & Medicinal Chemistry Letters 2016.0
Synthesis and structure–activity analysis of novel dihydropyridine derivatives to overcome multidrug resistance
Bioorganic & Medicinal Chemistry Letters 2001.0
Flavonoid-Related Modulators of Multidrug Resistance:  Synthesis, Pharmacological Activity, and Structure−Activity Relationships
Journal of Medicinal Chemistry 1999.0
New structure–activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR)
Bioorganic & Medicinal Chemistry 2013.0
Synthesis and bioevaluation of novel benzodipyranone derivatives as P-glycoprotein inhibitors for multidrug resistance reversal agents
European Journal of Medicinal Chemistry 2016.0