Development of nordihydroguaiaretic acid derivatives as potential multidrug-resistant selective agents for cancer treatment
2015
Huang, Lin-Chiang Sherlock | Chuang, Hong | Kapoor, Mohit | Hsieh, Cheng-Ying | Chou, Shih-Ching | Lin, Hui-Hsien | Chen, Yi-Wei | Chang, Chia-Ching | Hwu, Jih-Ru | Liang, Yu-Chuan | Xu, Minghua
In this research, we designed and synthesized a new series of nordihydroguaiaretic acid (NDGA) derivatives for multidrug resistance (MDR) research. A methylsulfonyl NDGA derivative, ((2R,3S)-2,3-dimethylbutane-1,4-diyl)bis(benzene-4,1,2-triyl) tetramethanesulfonate (5d), was found to inhibit MDR1 gene expression and suppress drug resistant MES-SA/Dx5 cells. Moreover, the combination of 5d and doxorubicin/terameprocol (M₄N) showed a profound synergistic effect on inhibition of drug resistant cancer cells, suggesting that 5d is a potential adjuvant applied with doxorubicin or terameprocol in cancer treatment.
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