Progesterone–adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux: Design, synthesis, characterization and biological evaluation

Steroids ◽  
2012 ◽  
Vol 77 (12) ◽  
pp. 1177-1191 ◽  
Author(s):  
Waël Zeinyeh ◽  
Zahia Mahiout ◽  
Sylvie Radix ◽  
Thierry Lomberget ◽  
Axel Dumoulin ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Multidrug Efflux ◽  
Design Synthesis ◽  
P Glycoprotein ◽  
Bivalent Inhibitors

Design, synthesis and evaluation of progesterone–adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux

2010 ◽  
Vol 20 (10) ◽  
pp. 3165-3168 ◽  
Author(s):  
Waël Zeinyeh ◽  
Ghina Alameh ◽  
Sylvie Radix ◽  
Catherine Grenot ◽  
Charles Dumontet ◽  
...  
Keyword(s):  
Multidrug Efflux ◽  
Design Synthesis ◽  
P Glycoprotein ◽  
Bivalent Inhibitors

Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness

2016 ◽  
Vol 88 (6) ◽  
pp. 820-831 ◽  
Author(s):  
Angela Stefanachi ◽  
Giuseppe Felice Mangiatordi ◽  
Piero Tardia ◽  
Domenico Alberga ◽  
Francesco Leonetti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Dft Studies ◽  
Design Synthesis ◽  
P Glycoprotein ◽  
Glycoprotein Inhibitors

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.

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.

Sign in / Sign up

Export Citation Format

Share Document