Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer

2021 ◽  
pp. 113775
Author(s):  
Dongdong Luo ◽  
Yuhang Zhang ◽  
Shuang Yang ◽  
Xiaochen Tian ◽  
Yan Lv ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Reversal Agents ◽  
Resistance Reversal ◽  
Sphingosine 1 Phosphate ◽  
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

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.

Design, synthesis and biological evaluation as immunosuppressant of amino alcohol derivatives containing thioether

2021 ◽  
Vol 11 (5) ◽  
pp. 773-780
Author(s):  
Yanjie Li ◽  
Yongqiang Li ◽  
Liu Yang ◽  
Zhi Liu ◽  
Ruimeng Zhang ◽  
...  
Keyword(s):  
Amino Alcohol ◽  
Coupling Reaction ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Suzuki Coupling Reaction ◽  
Sphingosine 1 Phosphate ◽  
Potential Activity ◽  
Key Steps ◽  
Synthesis And Biological Evaluation

To develop a safer immunosuppressant for organ transplantation and autoimmune disease treatment, in this study, several of novel amino alcohol derivatives containing thioether moiety were synthesized with 7-bromo-tetralin-2-one as starting material, and Suzuki coupling reaction and Bucherer-Bergs reaction as key steps. Their activity as sphingosine 1-phosphate receptor type 1 (S1P1) agonists were evaluated by [γ-35S] GTP binding assay. Among the thioether substituted compounds, compound 10 showed good activity as S1P1 agonist at low micromolar concentration (EC50 = 0.698 μmol/L). The result suggested that it has potential activity against autoimmune diseases and immunosuppressant of organ transplantations.

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.

Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents

2019 ◽  
Vol 161 ◽  
pp. 364-377 ◽  
Author(s):  
Xiao Wang ◽  
Qian-wen Ren ◽  
Xian-xuan Liu ◽  
Yan-ting Yang ◽  
Bing-hua Wang ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Biological Evaluation ◽  
Reversal Agents ◽  
Resistance Reversal ◽  
Synthesis And Biological Evaluation
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