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Discovery of napabucasin derivatives for the treatment of tuberculosis.

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机构： [1]Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, China. [2]State Key Laboratory of Respiratory Disease, Guangzhou Regenerative Medicine and Health Guangdong Laboratory (GRMH-GDL), Guangzhou Institutes of Biomedicine and Health (GIBH), Chinese Academy of Sciences (CAS) Guangzhou, 510530, China. [3]Institute of Physical Science and Information Technology, Anhui University, Hefei, 230601, China [4]University of Chinese Academy of Sciences (UCAS), Beijing, 100049, China [5]Laboratory of Human Diseases and Immunotherapies, West China Hospital, Sichuan University, Chengdu, Sichuan, China

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Tuberculosis is the contagious disease responsible for the highest number of deaths worldwide. Here, we screened a commercially available compound library and found napabucasin to possess a moderate anti-tubercular activity against M. tuberculosis H37Ra (MIC 2.5 μg mL-1, 10.4 μM). Three series of napabucasin derivatives were further evaluated for their in vitro anti-tubercular activities against Mtb H37Ra. The activity of most derivatives was either retained or enhanced compared with that of napabucasin. Compound 3s was the most active compound showing a MIC value of 0.3125 μg mL-1 (0.9 μM). Furthermore, several compounds were selected and evaluated against the Mtb H37Rv standard strain and six Mtb clinical isolates. Importantly, these compounds were found to be effective against Mtb clinical isolates with multi-resistance to isoniazid, rifampicin, and ethambutol. This journal is © The Royal Society of Chemistry 2019.

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出版当年[2019]版：

大类 | 4 区医学

小类 | 4 区生化与分子生物学 4 区药物化学

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第一作者机构： [1]Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, China.

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通讯机构： [2]State Key Laboratory of Respiratory Disease, Guangzhou Regenerative Medicine and Health Guangdong Laboratory (GRMH-GDL), Guangzhou Institutes of Biomedicine and Health (GIBH), Chinese Academy of Sciences (CAS) Guangzhou, 510530, China. [4]University of Chinese Academy of Sciences (UCAS), Beijing, 100049, China

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