期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 92, 期 3, 页码 1708-1716出版社
WILEY
DOI: 10.1111/cbdd.13338
关键词
click chemistry; MDR; P-gp inhibitor; reversal activity
资金
- National Natural Science Foundation of China [81673299]
- National Science and Technology Major Project of the Ministry of Science and Technology of China [2018ZX09301034-004, 2009ZX09102-033]
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells. Compound 19 also played an important role in the P-gp efflux function of intracellular Rh123 and doxorubicin (DOX) accumulation in K562/A02 cells. Moreover, compound 19 exhibited a long lifetime of approximately 24hr. These results indicated that compound 19 is a potential lead compound for the design of new drugs to overcome cancer MDR.
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