Trifluoromethylation/sulfonylation of alkynes from trifluoromethyl thianthrenium triflate and sulfur dioxide under extremely mild reaction conditions provides a facile access to trifluoromethyl-substituted vinyl sulfo...Trifluoromethylation/sulfonylation of alkynes from trifluoromethyl thianthrenium triflate and sulfur dioxide under extremely mild reaction conditions provides a facile access to trifluoromethyl-substituted vinyl sulfonohydrazides in moderate to good yields.This multicomponent reaction of trifluoromethyl thianthrenium triflate,alkynes,sulfur dioxide and hydrazines proceeds efficiently under visible light irradiation in the presence of photocatalyst at room temperature with broad substrate scope and excellent functional group compatibility.This reaction is highly stereoselective,and only(E)-isomers are obtained.Additionally,these trifluoromethyl-substituted vinyl sulfonohydrazides are further evaluated for anti-bacteria activity.In vitro activities of these compounds against Staphylococcus aureus(G+)and Escherichia coli(G-)are examined.展开更多
Osteosarcoma(OS)is the most common primary malignant bone tumor in children and adolescents.Although activator of HSP90 ATPase activity 1(AHA1)is reported to be a potential oncogene,its role in osteosarcoma progressio...Osteosarcoma(OS)is the most common primary malignant bone tumor in children and adolescents.Although activator of HSP90 ATPase activity 1(AHA1)is reported to be a potential oncogene,its role in osteosarcoma progression remains largely unclear.Since metabolism reprogramming is involved in tumorigenesis and cancer metastasis,the relationship between AHA1 and cancer metabolism is unknown.In this study,we found that AHA1 is significantly overexpressed in osteosarcoma and related to the prognosis of osteosarcoma patients.AHA1 promotes the growth and metastasis of osteosarcoma both in vitro and in vivo.Mechanistically,AHA1 upregulates the metabolic activity to meet cellular bioenergetic needs in osteosarcoma.Notably,we identifed that isocitrate dehydrogenase 1(IDH1)is a novel client protein of Hsp90 AHA1.Furthermore,the IDH1 protein level was positively correlated with AHA1 in osteosarcoma.And IDH1 overexpression could partially reverse the effect of AHA1 knockdown on cell growth and migration of osteosarcoma.Moreover,high IDH1 level was also associated with poor prognosis of osteosarcoma patients.This study demonstrates that AHA1 positively regulates IDH1 and metabolic activity to promote osteosarcoma growth and metastasis,which provides novel prognostic biomarkers and promising therapeutic targets for osteosarcoma patients.展开更多
A palladium-catalyzed [4+1] cycloaddition of prop-2-yn-1-ones with double isocyanides is developed herein.The transformation worked well to produce a series of 2-amino-4-cyanofurans with high efficiency and a broad re...A palladium-catalyzed [4+1] cycloaddition of prop-2-yn-1-ones with double isocyanides is developed herein.The transformation worked well to produce a series of 2-amino-4-cyanofurans with high efficiency and a broad reaction scope.Based on mechanism studies,it is believed that the palladiumcatalyzed [4+1] imidoylative cycloaddition of prop-2-yn-1-ones was concerted.Treated with a ryl amine and H_2 O,the [4+1] cycloaddition of prop-2-yn-1-ones with double isocyanides provided 2-amino-4-amidylpyrroles efficiently.展开更多
基金Financial support from National Natural Science Foundation of China(No.21871053)the Leading Innovative and Entrepreneur Team Introduction Program of Zhejiang(No.2019R01005)the Open Research Fund of School of Chemistry and Chemical Engineering,Henan Normal University(2020ZD04)。
文摘Trifluoromethylation/sulfonylation of alkynes from trifluoromethyl thianthrenium triflate and sulfur dioxide under extremely mild reaction conditions provides a facile access to trifluoromethyl-substituted vinyl sulfonohydrazides in moderate to good yields.This multicomponent reaction of trifluoromethyl thianthrenium triflate,alkynes,sulfur dioxide and hydrazines proceeds efficiently under visible light irradiation in the presence of photocatalyst at room temperature with broad substrate scope and excellent functional group compatibility.This reaction is highly stereoselective,and only(E)-isomers are obtained.Additionally,these trifluoromethyl-substituted vinyl sulfonohydrazides are further evaluated for anti-bacteria activity.In vitro activities of these compounds against Staphylococcus aureus(G+)and Escherichia coli(G-)are examined.
基金This work was supported by funds from the National Key Research and Development Program of China(No.2017YFA0505104)National Natural Science Foundation of China(Nos.81772540,81472506.81772861)+7 种基金the Science and Technology Program of Guangdong(No.2019A050510023)Guangdong Province Special Fund for Science and Technology Development(No.2017A050501015)Natural Science Foundation of Guangdong(Nos.2016A030313227,2018A030313689)the Science and Technology Program of Guangzhou(Nos.201704030008,201707010007)the Fundamental Research Funds for the Central Universities(No.19ykzd10)Cultivation of Major Projects,Sun Yat-sen University(No.80000-18823701)Cultivation of International Scientifhc Research Cooperation Platform.Sun Yat-sen University(No.800018827202)“3×3”Project,the First Afliated Hospital of Sun Yat-sen Universty(No.Y70215).
文摘Osteosarcoma(OS)is the most common primary malignant bone tumor in children and adolescents.Although activator of HSP90 ATPase activity 1(AHA1)is reported to be a potential oncogene,its role in osteosarcoma progression remains largely unclear.Since metabolism reprogramming is involved in tumorigenesis and cancer metastasis,the relationship between AHA1 and cancer metabolism is unknown.In this study,we found that AHA1 is significantly overexpressed in osteosarcoma and related to the prognosis of osteosarcoma patients.AHA1 promotes the growth and metastasis of osteosarcoma both in vitro and in vivo.Mechanistically,AHA1 upregulates the metabolic activity to meet cellular bioenergetic needs in osteosarcoma.Notably,we identifed that isocitrate dehydrogenase 1(IDH1)is a novel client protein of Hsp90 AHA1.Furthermore,the IDH1 protein level was positively correlated with AHA1 in osteosarcoma.And IDH1 overexpression could partially reverse the effect of AHA1 knockdown on cell growth and migration of osteosarcoma.Moreover,high IDH1 level was also associated with poor prognosis of osteosarcoma patients.This study demonstrates that AHA1 positively regulates IDH1 and metabolic activity to promote osteosarcoma growth and metastasis,which provides novel prognostic biomarkers and promising therapeutic targets for osteosarcoma patients.
基金Financial supports from the Natural Science Foundation of Shandong Province(Nos.ZR2019PB004 and ZR2018BB029)the Natural Science Foundation of China(Nos.21502069 and 21772067)are gratefully acknowledged。
文摘A palladium-catalyzed [4+1] cycloaddition of prop-2-yn-1-ones with double isocyanides is developed herein.The transformation worked well to produce a series of 2-amino-4-cyanofurans with high efficiency and a broad reaction scope.Based on mechanism studies,it is believed that the palladiumcatalyzed [4+1] imidoylative cycloaddition of prop-2-yn-1-ones was concerted.Treated with a ryl amine and H_2 O,the [4+1] cycloaddition of prop-2-yn-1-ones with double isocyanides provided 2-amino-4-amidylpyrroles efficiently.