Discovery of new pyrimidopyrrolizine/indolizine-based derivatives as P-glycoprotein inhibitors: design, synthesis, cytotoxicity, and MDR reversal activities

2021 ◽  
pp. 113403
Author(s):  
Ahmed M. Shawky ◽  
Ashraf N. Abdalla ◽  
Nashwa A. Ibrahim ◽  
Mohammed A.S. Abourehab ◽  
Ahmed M. Gouda
Keyword(s):  
Design Synthesis ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors ◽  
Mdr Reversal

Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness

2016 ◽  
Vol 88 (6) ◽  
pp. 820-831 ◽  
Author(s):  
Angela Stefanachi ◽  
Giuseppe Felice Mangiatordi ◽  
Piero Tardia ◽  
Domenico Alberga ◽  
Francesco Leonetti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Dft Studies ◽  
Design Synthesis ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

scholarly journals Tetrahydroquinolinone derivatives as potent P-glycoprotein inhibitors: design, synthesis, biological evaluation and molecular docking analysis

MedChemComm ◽  
2017 ◽  
Vol 8 (10) ◽  
pp. 1919-1933 ◽  
Author(s):  
S. Ranjbar ◽  
O. Firuzi ◽  
N. Edraki ◽  
O. Shahraki ◽  
L. Saso ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Phenyl Ring ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Docking Analysis ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors ◽  
Molecular Docking Analysis

Tetrahydroquinolinones bearing a phenyl ring with electron-withdrawing substitution showed remarkable P-glycoprotein inhibitory activity and significantly increased rhodamine accumulation in MES-SA/DX5 cells.

Status of Flavonols as P-Glycoprotein Inhibitors in Cancer Chemotherapy

2009 ◽  
Vol 5 (2) ◽  
pp. 89-99 ◽  
Author(s):  
Tripta Bansal ◽  
Manu Jaggi ◽  
Roop Khar ◽  
Sushama Talegaonkar
Keyword(s):  
Cancer Chemotherapy ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Chemosensitization potential of P-glycoprotein inhibitors in malaria parasites

2013 ◽  
Vol 134 (2) ◽  
pp. 235-243 ◽  
Author(s):  
Laura M. Alcantara ◽  
Junwon Kim ◽  
Carolina B. Moraes ◽  
Caio H. Franco ◽  
Kathrin D. Franzoi ◽  
...  
Keyword(s):  
Malaria Parasites ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

NEW 4-ARYL-1,4-DIHYDROPYRIDINES AND 4-ARYLPYRIDINES AS P-GLYCOPROTEIN INHIBITORS

2004 ◽  
Vol 33 (3) ◽  
pp. 321-328 ◽  
Author(s):  
Xiao-fei Zhou ◽  
Linping Zhang ◽  
Elaine Tseng ◽  
Elizabeth Scott-Ramsay ◽  
Jerome J. Schentag ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Glycoprotein Inhibitors

Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors

2021 ◽  
Vol 64 (19) ◽  
pp. 14895-14911
Author(s):  
Shuo Yuan ◽  
Bo Wang ◽  
Qing-Qing Dai ◽  
Xiao-Nan Zhang ◽  
Jing-Ya Zhang ◽  
...  
Keyword(s):  
P Glycoprotein ◽  
Quinazoline Derivatives ◽  
Orally Bioavailable ◽  
Glycoprotein Inhibitors

Effect of Clarithromycin on Steady-State Digoxin Concentrations

2003 ◽  
Vol 37 (2) ◽  
pp. 178-181 ◽  
Author(s):  
Hideko Tanaka ◽  
Kana Matsumoto ◽  
Kazuyuki Ueno ◽  
Mayumi Kodama ◽  
Kohji Yoneda ◽  
...  
Keyword(s):  
Heart Failure ◽  
Congestive Heart Failure ◽  
Digoxin Concentration ◽  
Concomitant Administration ◽  
Percentage Increase ◽  
P Glycoprotein ◽  
Before And After ◽  
Glycoprotein Inhibitors ◽  
Dose Dependent ◽  
Digoxin Therapy

OBJECTIVE: To evaluate the magnitude and dose-relatedness of the effect of clarithromycin on the pharmacokinetics of digoxin, and to compare the effects of clarithromycin with those of P-glycoprotein inhibitors. METHODS: Eight Japanese inpatients with congestive heart failure participated in this study. Each patient received oral digoxin therapy for at least 7 days and were coadministered oral clarithromycin to prevent or treat pneumonia. To evaluate the effects of clarithromycin on the pharmacokinetics of digoxin, digoxin concentrations were compared before and after coadministration of clarithromycin. RESULTS: Digoxin concentrations were higher after coadministration of clarithromycin in all patients (before, 0.838 ± 0.329 ng/mL; after, 1.36 ± 0.619 ng/mL); (p < 0.005). A significant correlation was observed between the dose of clarithromycin and the percentage of increase in the digoxin concentration. CONCLUSIONS: Digoxin concentrations increased during concomitant administration of clarithromycin, and this effect was dose-dependent on clarithromycin. The percentage increase in digoxin concentrations after the usual oral dose of clarithromycin (400 mg/d) is approximately 70%. Therefore, digoxin concentrations must be monitored carefully after coadministration of clarithromycin, and the doses of digoxin may need readjustment in patients who are concomitantly receiving clarithromycin.

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