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Advances in Enantioselective Construction of Trifluoromethoxylated Stereogenic Carbon Centers

Chinese Journal of Chemistry 2020年第1期38卷 101-102页

作者： Xiaohuan Jiang Pingping Tang State Key Laboratory and Institute of Elemento-Organic Chemistry College of ChemistryNankai UniversityTianjin 300071China

In recent years,the trifluoromethoxy(OCF3)functional group has received extensive attention in phar-maceuticals,agrochemicals and material ***,the methods for the enantioselective syn-thesis of trifluoromethoxylated stereogenic carbon centers are rare owing to the nature of easy decom-position of OCF3 anion and limited OCF3 *** the asymmetric trifluoromethoxylation will be a hot research topic in near future due to the unique biological properties of a single *** article mainly focuses on the recent advances in the enantioselectiveconstruction of trifluoromethoxylated stereogenic carbon centers.

关键词： methoxyl reagent centers

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Co-delivery of resveratrol and docetaxel via polymeric micelles to improve the treatment of drug-resistant tumors

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Asian Journal of Pharmaceutical Sciences 2019年第1期14卷 78-85页

作者： Xiong Guo Zhiyue Zhao Dawei Chen Mingxi Qiao Feng Wan Dongmei Cun Yi Sun Mingshi Yang Wuya College of Innovation Shenyang Pharmaceutical UniversityWenhua Road No.103Shenyang 110016China School of Graduate Liaoning University of Traditional Chinese MedicineChong Shan Road No.79Shenyang 110847China School of Pharmacy Shenyang Pharmaceutical UniversityWenhua Road No.103Shenyang 110016China Department of Pharmacy Faculty of Health and Medical SciencesUniversity of CopenhagenUniversitetsparken 2DK-2100 Copenhagen ODenmark Department of Micro-and Nanotechnology Technical University of Denmarkφsteds PladsKgs.Lyngby 2800Denmark

Co-delivery of anti-cancer drugs is promising to improve the efficacy of cancer *** study was aiming to investigate the potential of concurrent delivery of resveratrol(RES)and docetaxel(DTX)via polymeric nanocarriers to treat breast *** this end,methoxyl poly(ethylene glycol)-poly(D,L-lactide)copolymer(mPEG-PDLA)was prepared and characterized using FTIR and 1H NMR,and their molecular weights were determined by *** analysis and combination index calculation were performed to find the optimal ratio between RES and DTX to against human breast adenocarcinoma cell line(MCF-7 cells).Subsequently,RES and DTX were loaded in the mPEG-PDLA micelles simultaneously,and the morphology,particle size distribution,in vitro release,pharmacokinetic profiles,as well as cytotoxicity to the MCF-7 cells were ***50 of RES and DTX in MCF-7 cells were determined to be 23.0μg/ml and 10.4μg/ml,respectively,while a lower IC50 of 4.8μg/ml of the combination of RES and DTX was *** combination of RES and DTX at a ratio of 1:1(w/w)generated stronger synergistic effect than other ratios in the MCF-7 *** and DTX loaded mPEG-PDLA micelles exhibited prolonged release profiles,and enhanced cytotoxicity in vitro against MCF-7 *** AUC(0→t)of DTX and RES in mPEG-PDLA micelles after *** to rats were 3.0-fold and 1.6-fold higher than that of *** of the individual *** findings indicated that the co-delivery of RES and DTX using mPEG-PDLA micelles could have better treatment of tumors.

关键词： Resveratrol Docetaxel methoxyl poly(ethylene glycol)-poly(d,l-lactide)copolymer (mPEG-PDLA) Micelles Drug resistance tumor

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