Synthesis and Biological Evaluation of (Hetero)Arylmethyloxy- and Arylmethylamine-phenyl Derivatives as Potent P-glycoprotein Modulating Agents

2008 ◽  
Vol 51 (5) ◽  
pp. 1415-1422 ◽  
Author(s):  
Nicola Antonio Colabufo ◽  
Francesco Berardi ◽  
Roberto Perrone ◽  
Simona Rapposelli ◽  
Maria Digiacomo ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
P Glycoprotein ◽  
Synthesis And Biological Evaluation

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

scholarly journals Synthesis and Biological Evaluation of New 3,4-diarylmaleimides as Enhancers (modulators) of Doxorubicin Cytotoxic Activity on Cultured Tumor Cells from a Real Case of Breast Cancer

2017 ◽  
Vol 61 (1) ◽  
Author(s):  
Jessica R. Gutierrez-Cano ◽  
Pradip D. Nahide ◽  
Velayudham Ramadoss ◽  
Yuvraj Satkar ◽  
Rafael Ortiz-Alvarado ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cultured Cells ◽  
Biological Evaluation ◽  
Doxorubicin Treatment ◽  
P Glycoprotein ◽  
Molecular Action ◽  
Mortality Effect ◽  
Kinase Phosphorylation ◽  
Synthesis And Biological Evaluation ◽  
Cultured Tumor Cells

<p>A series of new 3,4-diarylmaleimides were synthesized in an optimized and efficient lineal sequence of three steps, starting from commercial maleimide. The biological evaluation of these compounds as enhancers (activity modulators) in the co-administration with doxorubicin treatment in breast cancer cells directly obtained from a patient, were essayed. The cancerous tissue BT026-512N was provided by the National Institute of Cancerology (INCAN) of México. This tissue was obtained by biopsy from a patient diagnosed with stage IIB ductal breast cancer. The results obtained in the assays, show decreased cell viability on the cultured cells for all of the maleimides synthesized in combinatorial administration with doxorubicin. The highest mortality effect was determined for maleimides <strong>9</strong> and <strong>29</strong> increased in close to three times the effect compared with treatment using only doxorubicin. Based on previous functionalized maleimides core reports and Molinspiration chemoinformatic analysis, these results could possibly point out to the Pg-p glycoprotein as bio-molecular action target of maleimides by kinase phosphorylation-inhibition, although more experimental data is necessary.</p>

Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors

2020 ◽  
Vol 201 ◽  
pp. 112422
Author(s):  
Chin-Chuan Hung ◽  
Chien-Yu Chen ◽  
Yu-Chieh Wu ◽  
Chien-Fu Huang ◽  
Yu-Chun Huang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis, and Biological Evaluation of (S)-Valine Thiazole-Derived Cyclic and Noncyclic Peptidomimetic Oligomers as Modulators of Human P-Glycoprotein (ABCB1)

ChemBioChem ◽  
2013 ◽  
Vol 15 (1) ◽  
pp. 157-169 ◽  
Author(s):  
Satyakam Singh ◽  
Nagarajan Rajendra Prasad ◽  
Khyati Kapoor ◽  
Eduardo E. Chufan ◽  
Bhargav A. Patel ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
P Glycoprotein ◽  
Synthesis And Biological Evaluation

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.

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