Browsing by Author "Lin, Hui-Hsien"

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Development of nordihydroguaiaretic acid derivatives as potential multidrug-resistant selective agents for cancer treatment
(2015-01-01)
Huang, Lin-Chiang Sherlock
;
Chuang, Hong
;
Kapoor, Mohit
;
Hsieh, Cheng-Ying
;
Chou, Shih-Ching
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 resistantMES-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.
Synthesis and Evaluation of Aminothiazole-Paeonol Derivatives as Potential Anticancer Agents
(2016-02-01)
Tsai, Chia-Ying
;
Kapoor, Mohit
;
Huang, Ying-Pei
;
Lin, Hui-Hsien
;
Liang, Yu-Chuan
In this study, novel aminothiazole-paeonol derivatives were synthesized and characterized using H-1-NMR, C-13-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the new synthesized compounds were evaluated according to their anticancer effect on seven cancer cell lines. The experimental results indicated that these compounds possess high anticancer potential regarding human gastric adenocarcinoma (AGS cells) and human colorectal adenocarcinoma (HT-29 cells). Among these compounds, N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]-4-methoxybenzenesulfonamide (13c) had the most potent inhibitory activity, with IC50 values of 4.0 mu M to AGS, 4.4 mu M to HT-29 cells and 5.8 mu M to HeLa cells. The 4-fluoro-N-[4-(2-hydroxy-4-methoxyphenyl)thiazol-2-yl]benzenesulfonamide (13d) was the second potent compound, showing IC50 values of 7.2, 11.2 and 13.8 mu M to AGS , HT-29 and HeLa cells, respectively. These compounds are superior to 5-fluorouracil (5-FU) for relatively higher potency against AGS and HT-29 human cancer cell lines along with lower cytotoxicity to fibroblasts. Novel aminothiazole-paeonol derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating gastrointestinal adenocarcinoma.