Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters

2014 ◽  
Vol 87 ◽  
pp. 398-412 ◽  
Author(s):  
Silvia Dei ◽  
Marcella Coronnello ◽  
Elisa Floriddia ◽  
Gianluca Bartolucci ◽  
Cristina Bellucci ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
High Activity ◽  
Alkanol Amine

Novel dithiane analogues of tiapamil with high activity to overcome multidrug resistance in vitro

1995 ◽  
Vol 50 (2) ◽  
pp. 187-196 ◽  
Author(s):  
James F. Eliason ◽  
Henri Ramuz ◽  
Takashi Yoshikubo ◽  
Tohru Ishikawa ◽  
Taeko Yamamoto ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
High Activity

Structure−Activity Relationships Studies in a Series ofN,N-Bis(alkanol)amine Aryl Esters as P-Glycoprotein (Pgp) Dependent Multidrug Resistance (MDR) Inhibitors†

2010 ◽  
Vol 53 (4) ◽  
pp. 1755-1762 ◽  
Author(s):  
Cecilia Martelli ◽  
Marcella Coronnello ◽  
Silvia Dei ◽  
Dina Manetti ◽  
Francesca Orlandi ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
P Glycoprotein ◽  
Alkanol Amine

scholarly journals Dual P-Glycoprotein and CA XII Inhibitors: A New Strategy to Reverse the P-gp Mediated Multidrug Resistance (MDR) in Cancer Cells

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1748 ◽  
Author(s):  
Elisabetta Teodori ◽  
Laura Braconi ◽  
Silvia Bua ◽  
Andrea Lapucci ◽  
Gianluca Bartolucci ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Cells ◽  
Glycoprotein P ◽  
Reversal Effect ◽  
P Glycoprotein ◽  
New Strategy ◽  
Uptake Test ◽  
New Compounds ◽  
Alkanol Amine ◽  
Mdr Reversal

A new series of N,N-bis(alkanol)amine aryl diesters was synthesized and studied as dual P-glycoprotein (P-gp) and carbonic anhydrase XII inhibitors (CA XII). These hybrids should be able to synergistically overcome P-gp mediated multidrug resistance (MDR) in cancer cells. It was reported that the efflux activity of P-gp could be modulated by CA XII, as the pH reduction caused by CA XII inhibition produces a significant decrease in P-gp ATPase activity. The new compounds reported here feature both P-gp and CA XII binding moieties. These hybrids contain a N,N-bis(alkanol)amine diester scaffold found in P-glycoprotein ligands and a coumarin or benzene sulfonamide moiety to target CA XII. Many compounds displayed a dual activity against P-gp and CA XII being active in the Rhd 123 uptake test on K562/DOX cells and in the hCA XII inhibition test. On LoVo/DOX cells, that overexpress both P-gp and CA XII, some coumarin derivatives showed a high MDR reversal effect in Rhd 123 uptake and doxorubicin cytotoxicity enhancement tests. In particular, compounds 7 and 8 showed higher activity than verapamil and were more potent on LoVo/DOX than on K562/DOX cells overexpressing only P-gp. They can be considered as valuable candidates for selective P-gp/CA XII inhibition in MDR cancer cells.

scholarly journals Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated membrane ATPase.

1992 ◽  
Vol 267 (7) ◽  
pp. 4854-4858 ◽  
Author(s):  
B Sarkadi ◽  
E.M. Price ◽  
R.C. Boucher ◽  
U.A. Germann ◽  
G.A. Scarborough
Keyword(s):  
Multidrug Resistance ◽  
High Activity ◽  
Insect Cells ◽  
Membrane Atpase

Study of the mechanism responsible for multidrug resistance in breast cancer MCF-7 cell mediated by 14-3-3σ

2010 ◽  
Vol 34 (8) ◽  
pp. S47-S47
Author(s):  
Guopei Zheng ◽  
Sisi Yi ◽  
Yafei Li ◽  
Fangren Kong ◽  
Yanhui Yu ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Mcf 7

Expression and localization of the multidrug resistance proteins MRP2 and MRP3 in human gallbladder epithelia

2001 ◽  
Vol 120 (5) ◽  
pp. A93-A93
Author(s):  
D ROST ◽  
J KONIG ◽  
G WEISS ◽  
E KLAR ◽  
W STREMMEL ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Multidrug Resistance Proteins ◽  
Human Gallbladder ◽  
Resistance Proteins
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