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European journal of medicinal chemistry v.143, 2018년, pp.1535 - 1542   SCI SCIE
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Exploration of 1,2,3-triazole-pyrimidine hybrids as potent reversal agents against ABCB1-mediated multidrug resistance

Wang, Bo (Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China ) ; Zhao, Bing (Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China ) ; Chen, Zhe-Sheng (Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, USA ) ; Pang, Lu-Ping (Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry o ) ; Zhao, Yuan-Di ; Guo, Qian ; Zhang, Xin-Hui ; Liu, Ying ; Liu, Guang-Yao ; Hao-Zhang, Guang-Yao ; Zhang, Xin-Yuan ; Ma, Li-Ying ; Liu, Hong-Min ;
  • 초록  

    Abstract ABCB1-mediated multidrug resistance (MDR) is a principal obstacle for successful cancer chemotherapy. A series of pyrimidine-based hybrid molecules containing 1,2,3-triazole moiety were evaluated for their reversal activities against MDR. The majority of target compounds displayed moderate to great reversal potency. Among these compounds, compound 25 displayed the most potent reversal activity, about 7-fold more potent than Verapamil (VRP). Further mechanism studies revealed that compound 25 could obviously reverse paclitaxel (PTX) resistance in SW620/AD300 cells by increasing accumulation and extending maintenance of PTX. Our findings indicate that the 1,2,3-triazole-pyrimidine-based derivatives may serve as an interesting lead for the development of new potent and efficacious ABCB1-dependent MDR modulators. Highlights Serial pyrimidine derivatives were evaluated reversal activity against MDR. Most compounds displayed moderate to great reversal potency. Compound 25 displayed the best reversal activity, about 7-fold more potent than VRP. Compound 25 significantly increased the concentration of cellular PTX. Graphical abstract [DISPLAY OMISSION]


  • 주제어

    Pyrimidine .   1,2,3-Triazole .   Paclitaxel (PTX) .   MDR reverser .   ABCB1 modulator.  

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