Synthesis and evaluation of substituted dibenzo[c,e]azepine-5-ones as P-glycoprotein-mediated multidrug resistance reversal agents

2012 ◽  
Vol 22 (8) ◽  
pp. 2675-2680 ◽  
Author(s):  
Xiaobo Tang ◽  
Xiaoke Gu ◽  
Zhiguang Ren ◽  
Yuanfang Ma ◽  
Yisheng Lai ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Resistance Reversal

Design, Synthesis and Biological Evaluation of Dimethyl Cardamonin (DMC) Derivatives as P-glycoprotein-mediated Multidrug Resistance Reversal Agents

2020 ◽  
Vol 17 (10) ◽  
pp. 1270-1282
Author(s):  
Ximeng Shi ◽  
Yuyu Zhao ◽  
Licheng Zhou ◽  
Huanhuan Yin ◽  
Jianwen Liu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Biological Evaluation ◽  
Glycoprotein P ◽  
Design Synthesis ◽  
Reversal Agents ◽  
Protein Levels ◽  
P Glycoprotein ◽  
Resistance Reversal ◽  
Mcf 7

Background: P-glycoprotein (P-gp) has been regarded as an important factor in the multidrug resistance (MDR) of tumor cells within the last decade, which can be solved by inhibiting Pgp to reverse MDR. Thus, it is an effective strategy to develop inhibitor of P-gp. Objective: In this study, the synthesis of a series of derivatives had been carried out by bioisosterism design on the basis of Dimethyl Cardamonin (DMC). Subsequently, we evaluated their reversal activities as potential P-glycoprotein (P-gp)-mediated Multidrug Resistance (MDR) agents. Methods: Dimethyl cardamonin derivatives were synthesized from acetophenones and the corresponding benzaldehydes in the presence of 40% KOH by Claisen-Schmidt reaction. Their cytotoxicity and reversal activities in vitro were assessed with MTT. Moreover, the compound B4 was evaluated by Doxorubicin (DOX) accumulation, Western blot and wound-healing assays deeply. Results and Conclusion: The results showed that compounds B2, B4 and B6 had the potency of MDR reversers with little intrinsic cytotoxicity. Meanwhile, these compounds also demonstrated the capability to inhibit MCF-7 and MCF-7/DOX cells migration. Besides, the most compound B4 was selected for further study, which promoted the accumulation of DOX in MCF-7/DOX cells and inhibited the expressionof P-gp at protein levels. Conclusion: The above findings may provide new insights for the research and development of Pgp- mediated MDR reversal agents.

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

2014 ◽  
Vol 22 (24) ◽  
pp. 6857-6866 ◽  
Author(s):  
Lei Jiao ◽  
Qianqian Qiu ◽  
Baomin Liu ◽  
Tianxiao Zhao ◽  
Wenlong Huang ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Design Synthesis ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Resistance Reversal

Synthesis and Biological Evaluation of C-Aromataxane Derivatives as P-Glycoprotein-Mediated Multi Drug Resistance Reversal Agents

Heterocycles ◽  
2015 ◽  
Vol 90 (1) ◽  
pp. 482
Author(s):  
Takayuki Doi ◽  
Naoko Yamaguchi ◽  
Kosuke Ohsawa ◽  
Kazuoki Nakai ◽  
Masahito Yoshida ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Biological Evaluation ◽  
Multi Drug Resistance ◽  
Reversal Agents ◽  
P Glycoprotein ◽  
Resistance Reversal ◽  
Synthesis And Biological Evaluation

Multidrug Resistance Reversal Agents

ChemInform ◽  
2004 ◽  
Vol 35 (6) ◽  
Author(s):  
Jacques Robert ◽  
Christian Jarry
Keyword(s):  
Multidrug Resistance ◽  
Reversal Agents ◽  
Resistance Reversal
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