Browsing by Author "Huang, Lin-Chiang Sherlock"

Now showing 1 - 2 of 2

Design and synthesis of pyridine-pyrazole-sulfonate derivatives as potential anti-HBV agents
(2016)
Chuang, Hong
;
Huang, Lin-Chiang Sherlock
;
Kapoor, Mohit
;
Liao, Yi-Jen
;
Yang, Cheng-Lin
Hepatitis B virus (HBV) is an infectious disease, which can cause acute and chronic infections. Every year, over 7.5 million persons die due to HBV. No effective drug exists for the treatment of HBV. Thus, we designed and synthesized 16 new pyridine-pyrazole-sulfonate compounds containing pyridine-SCH2-pyrazole and pyridine-pyrazole derivatives. Their structures were characterized by H-1-NMR, C-13-NMR, IR, mass spectroscopy, and high performance liquid chromatography. All the compounds were evaluated for their anti-HBV activities and a structure-activity relationship (SAR) in HepG2 2.2.15 cells was established. We found that the pyridine-pyrazole derivatives could inhibit the HBV gene expression and viral DNA replication. Among these compounds, 2-[3-(2-nitrophenylsulfonyl)oxy-5-pyrazol-yl]pyridine 19d has shown the most potent inhibitory activity with an IC50 value of 9.19 mu M and high selectivity index, SI (TC50/IC50) of 35.46. Hence, we believe our compounds could serve as a potential lead compounds for anti-HBV drug development.
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.