A method for stereoselective construction of Z-monofluoroalkenes by nickel-catalyzed defluorinative coupling of gem‑difluoroalkenes in mild conditions was described.The combination of lithium organoborate and ZnBr_(2)...A method for stereoselective construction of Z-monofluoroalkenes by nickel-catalyzed defluorinative coupling of gem‑difluoroalkenes in mild conditions was described.The combination of lithium organoborate and ZnBr_(2) generated in situ lithium aryl zincates,which facilitates the transmetalation step of the nickel-catalyzed cross coupling reaction.展开更多
Gambogic acid(GA) is a natural substance with a good antitumor effect, but it is too lipophilic to be metabolized and excreted, thus accumulating in the body. Gemcitabine(GEM), one of the first-line antitumor drugs, h...Gambogic acid(GA) is a natural substance with a good antitumor effect, but it is too lipophilic to be metabolized and excreted, thus accumulating in the body. Gemcitabine(GEM), one of the first-line antitumor drugs, has high hydrophilicity, which greatly shortens its half-life in vivo. We previously reported a compound named N-gamboyl gemcitabine(GAG), derived from the condensation of GEM and GA, whose hydrophilicity is better than GA and stability is better than GEM. Here, the antitumor performance of GAG was investigated for the first time by using several common tumor cell lines as tumor models. The results of in vitro study showed that GAG significantly inhibited the proliferation and migration of the tumor cells. The IC50 values of GAG for the tumor cells were lower than those of GEM and GA. The present study suggests that GAG has a promising potential to be developed into a broad-spectrum antitumor drug.展开更多
基金the National Natural Science Foundation of China(Nos.21625206.21632009,21421002,22061160465)for financial support.
文摘A method for stereoselective construction of Z-monofluoroalkenes by nickel-catalyzed defluorinative coupling of gem‑difluoroalkenes in mild conditions was described.The combination of lithium organoborate and ZnBr_(2) generated in situ lithium aryl zincates,which facilitates the transmetalation step of the nickel-catalyzed cross coupling reaction.
基金Science&Technology Commission of Shanghai MunicipalityChina (No.20DZ2254900)+3 种基金Municipal Public Welfare Research Project from JiaxingZhejiang ProvinceChina (No.2022AY10001)Open Project Program of Jiaxing Key Laboratory of Virus-Related Infectious Diseases。
文摘Gambogic acid(GA) is a natural substance with a good antitumor effect, but it is too lipophilic to be metabolized and excreted, thus accumulating in the body. Gemcitabine(GEM), one of the first-line antitumor drugs, has high hydrophilicity, which greatly shortens its half-life in vivo. We previously reported a compound named N-gamboyl gemcitabine(GAG), derived from the condensation of GEM and GA, whose hydrophilicity is better than GA and stability is better than GEM. Here, the antitumor performance of GAG was investigated for the first time by using several common tumor cell lines as tumor models. The results of in vitro study showed that GAG significantly inhibited the proliferation and migration of the tumor cells. The IC50 values of GAG for the tumor cells were lower than those of GEM and GA. The present study suggests that GAG has a promising potential to be developed into a broad-spectrum antitumor drug.
