ChemInform Abstract: Design, Synthesis and Evaluation of Substituted N-(3-Arylpropyl)-9,10-dihydro-9-oxoacridine-4-carboxamides as Potent MDR Reversal Agents in Cancer.

ChemInform ◽  
2011 ◽  
Vol 42 (28) ◽  
pp. no-no
Author(s):  
V. S. Velingkar ◽  
V. D. Dandekar
Keyword(s):  
Design Synthesis ◽  
Reversal Agents ◽  
Mdr Reversal

Design and Syntheses of Permethyl Ningalin B Analogues: Potent Multidrug Resistance (MDR) Reversal Agents of Cancer Cells

2010 ◽  
Vol 53 (14) ◽  
pp. 5108-5120 ◽  
Author(s):  
Pu Yong Zhang ◽  
Iris L. K. Wong ◽  
Clare S. W. Yan ◽  
Xiao Yu Zhang ◽  
Tao Jiang ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Cells ◽  
Reversal Agents ◽  
Mdr Reversal

Design, synthesis and biological evaluation of novel triazole-core reversal agents against P-glycoprotein-mediated multidrug resistance

RSC Advances ◽  
2016 ◽  
Vol 6 (31) ◽  
pp. 25819-25828 ◽  
Author(s):  
Bo Zhang ◽  
Tianxiao Zhao ◽  
Jie Zhou ◽  
Qianqian Qiu ◽  
Yuxuan Dai ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Click Chemistry ◽  
Biological Evaluation ◽  
Glycoprotein P ◽  
Design Synthesis ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Synthesis And Biological Evaluation

We designed and synthesized a novel series of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) inhibitors bearing a triazolphenethyl–tetrahydroisoquinoline scaffold through click chemistry.

A CONVENIENT ROUTE TO 1,4-DIHYDRO-3-CYANO-10-METHYL-PYRIDO[3,2-g)-QUINOLINE DERIVATIVES AS KEY-INTERMEDIATES FOR THE SYNTHESIS OF NOVEL MDR REVERSAL AGENTS

2004 ◽  
Vol 10 (1) ◽  
Author(s):  
Claudia MOLDOVAN ◽  
Castelia CRISTEA ◽  
loan A.SILBERG ◽  
Abdallah MARAMOUD ◽  
Calin DELEANU ◽  
...  
Keyword(s):  
Quinoline Derivatives ◽  
Reversal Agents ◽  
Convenient Route ◽  
Mdr Reversal

Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype

Blood ◽  
1992 ◽  
Vol 80 (6) ◽  
pp. 1528-1536 ◽  
Author(s):  
RJ Arceci ◽  
K Stieglitz ◽  
BE Bierer
Keyword(s):  
Efflux Pump ◽  
Multidrug Resistant ◽  
Chemotherapeutic Agents ◽  
Cytotoxic Drug ◽  
Cytotoxic Agents ◽  
Cross Resistance ◽  
Clinical Role ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Mdr Reversal

Abstract The multidrug-resistant (MDR) phenotype is characterized in vitro by the resistance displayed by cell lines to a broad spectrum of natural product cytotoxic agents. This high level of cross-resistance is due to the increased expression of a membrane glycoprotein termed P- glycoprotein. Encoded in humans by the mdr1 gene, P-glycoprotein functions as an energy-dependent efflux pump of these cytotoxic agents. In this report, we demonstrate that the newly characterized immunosuppressant FK506 and its structural analogue, rapamycin, are capable of functioning as MDR reversal agents. FK506 and rapamycin increase both intracellular, cytotoxic drug (daunomycin) accumulation, and the cytotoxicity of chemotherapeutic agents in multidrug-resistant cells. The increase in cytotoxic drug accumulation is observed at concentrations of FK506 and rapamycin 1,000-fold greater than the concentrations required for FK506 and rapamycin to inhibit T-lymphocyte activation and similar to those shown to be effective for other MDR reversal agents such as cyclosporine A (CsA) and verapamil. The effect of FK506 or rapamycin on both intracellular accumulation and cytotoxicity of daunomycin is additive. This is supported by the ability of FK506 and rapamycin to directly compete the binding of the photoaffinity analogue 125I-iodoaryl azidoprazosin to the P- glycoprotein. The data demonstrate that FK506 and rapamycin represent a new class of structurally distinct molecules that can function as MDR reversal agents and suggest a previously unidentified, potential clinical role for these compounds.

Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells

2012 ◽  
Vol 22 (2) ◽  
pp. 801-805 ◽  
Author(s):  
Xiaobo Tang ◽  
Xiaoke Gu ◽  
Hua Ai ◽  
Guangji Wang ◽  
Hui Peng ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Reversal Agents ◽  
Nitric Oxide Releasing ◽  
Mdr Reversal ◽  
Mcf 7
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