Browsing by Author "Chuang, Hong"

Now showing 1 - 4 of 4

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.
Directly Thiolated Modification onto the Surface of Detonation Nanodiamonds
(2014-05-28)
Hsu, Ming-Hua
;
Chuang, Hong
;
Cheng, Fong-Yu
;
Huang, Ying-Pei
;
Han, Chien-Chung
An efficient method for modifying the surface of detonation nanodiamonds (5 and 100 nm) with thiol groups (-SH) by using an organic chemistry strategy is presented herein. Thiolated nanodiamonds were characterized by spectroscopic techniques, and the atomic percentage of sulfur was analyzed by elemental analysis and X-ray photoelectron spectroscopy. The conjugation between thiolated nanodiamonds and gold nanoparticles was elucidated by transmission electron microscopy and UV-vis spectrometry. Moreover, the material did not show significant cytotoxicity to the human lung carcinoma cell line and may prospectively be applied in bioconjugated technology. The new method that we elucidated may significantly improve the approach to surface modification of detonation nanodiamonds and build up a new platform for the application of nanodiamonds.
Simple and highly efficient direct thiolation of the surface of carbon nanotubes
(2014)
Hsu, Ming-Hua
;
Chuang, Hong
;
Cheng, Fong-Yu
;
Huang, Ying-Pei
;
Han, Chien-Chung
We established a highly efficient and simple method to directly functionalize the surface of carbon nanotubes (CNTs) with thiol groups (-SH). The -SH groups on the surface of the CNTs were characterized using Raman spectroscopy, X-ray photoelectron spectroscopy (XPS), elemental analysis (EA), and transmission electron microscopy (TEM). The TEM indicated that gold nanoparticles (Au NPs) or other metals can be attached to thiolated CNTs (CNT-SHs) through thiol-metal bonding. Hence, the proposed approach can be used for developing self-assembled materials, sensors, catalysts, and CNT nanodevices.