- Design, Synthesis, Molecular Docking, and Biological Evaluation of New Emodin Anthraquinone Derivatives as Potential Antitumor Substances
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The emodin anthraquinone derivatives are generally used in traditional Chinese medicine due to their various pharmacological activities. In the present study, a series of emodin anthraquinone derivatives have been designed and synthesized, among which 1,3-dihydroxy-6,8-dimethoxyanthracene-9,10-dione is a natural compound that has been synthesized for the very first time, and 1,3-dimethoxy-5,8-dimethylanthracene-9,10-dione is a compound that has never been reported earlier. Interestingly, while total seven of these compounds showed neuraminidase inhibitory activity in influenza virus with inhibition rate more than 50 %, specific four compounds exhibited significant inhibition of tumor cell proliferation. The further results demonstrate that 1,3-dimethoxy-5,8-dimethylanthracene-9,10-dione showed the best anticancer activity among all the synthesized compounds by inducing highest apoptosis rate to HCT116 cancer cells and arresting their G0/G1 cell cycle phase, through elevation of intracellular level of reactive oxygen species (ROS). Moreover, the binding of 1,3-dimethoxy-5,8-dimethylanthracene-9,10-dione with BSA protein has thoroughly been investigated. Altogether, this study suggests the neuraminidase inhibitory activity and antitumor potential of the new emodin anthraquinone derivatives.
- Li, Yuying,Guo, Fang,Chen, Tinggui,Zhang, Liwei,Wang, Zhuanhua,Su, Qiang,Feng, Liheng
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- Method for synthesizing 3,5-dimethoxy-phthalic anhydride as medicine intermediate
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The invention provides a method for synthesizing 3,5-dimethoxy-phthalic anhydride as a medicine intermediate. The method includes the steps of firstly adding a certain amount of methyl 3,5-dimethoxybenzoate and chloral hydrate into a four-necked bottle, a
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Paragraph 0006
(2018/03/24)
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- Synthesis and biological activity of new phthalimides as potential anti-inflammatory agents
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The overproduction of nitric oxide (NO) plays an important role in a variety of pathophysiological processes, including inflammation. Therefore, the suppression of NO production is a promising target in the design of anti-inflammatory agents. In the prese
- Bach, Duc-Hiep,Liu, Jian-Yu,Kim, Won Kyung,Hong, Ji-Young,Park, So Hyun,Kim, Donghwa,Qin, Si-Ning,Luu, Thi-Thu-Trang,Park, Hyen Joo,Xu, Yong-Nan,Lee, Sang Kook
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p. 3396 - 3405
(2017/05/29)
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