The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are po...The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.展开更多
3-CF3 S substituted thioflavones and benzothiophenes were achieved via the reactions of AgSCF3 with methylthiolated alkynones and alkynylthioanisoles,respectively,promoted by persulfate.This protocol possesses good fu...3-CF3 S substituted thioflavones and benzothiophenes were achieved via the reactions of AgSCF3 with methylthiolated alkynones and alkynylthioanisoles,respectively,promoted by persulfate.This protocol possesses good functional group tolerance and high yields.Mechanistic studies suggested that a classic two-step radical process was involved,which includes addition of CF3 S radical to triple bond and cyclization with SMe moiety.展开更多
A novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71(EV71)and the coxsackievirus B3(CVB3)and B6(CVB6)were evaluated.Compounds 7d and 9b showed ...A novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71(EV71)and the coxsackievirus B3(CVB3)and B6(CVB6)were evaluated.Compounds 7d and 9b showed potent antiviral activities against EV71 with ICso values of 8.27 and 5.48μM,respectively.Compound 7f,which has been synthesized for the first time in this work,showed the highest level of inhibitory activity against both CVB3 and CVB6 with an ICso value of 0.62 and 0.87μM.Compounds 4b,7a,9c and 9e also showed strong inhibitory activities against both the CVB3 and CV B6 at low concentrations(IC_(50)=1.42-7.15μM),whereas compounds 4d,7c,7e and 7g showed strong activity against CVB6(IC_(50)=2.91-3.77μM)together with low levels of activity against CVB3.Compound 7d exhibited stronger inhibitory activity against CVB3(IC_(50)=6.44μM)thaln CVB6(IC_(50)>8.29μM).The thioflavone derivatives 7a,7c,7d,7e,7f and 7g,represent a new class of lead compounds for the development of novel antiviral agents.展开更多
文摘The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.
基金the National Natural Science Foundation of China(Nos.21991123,21677094)for financial support。
文摘3-CF3 S substituted thioflavones and benzothiophenes were achieved via the reactions of AgSCF3 with methylthiolated alkynones and alkynylthioanisoles,respectively,promoted by persulfate.This protocol possesses good functional group tolerance and high yields.Mechanistic studies suggested that a classic two-step radical process was involved,which includes addition of CF3 S radical to triple bond and cyclization with SMe moiety.
基金This work was supported by the National Science and Technology Major Special Project for Major New Drugs Innovation(Item Number:2012ZX09102-101-001).
文摘A novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71(EV71)and the coxsackievirus B3(CVB3)and B6(CVB6)were evaluated.Compounds 7d and 9b showed potent antiviral activities against EV71 with ICso values of 8.27 and 5.48μM,respectively.Compound 7f,which has been synthesized for the first time in this work,showed the highest level of inhibitory activity against both CVB3 and CVB6 with an ICso value of 0.62 and 0.87μM.Compounds 4b,7a,9c and 9e also showed strong inhibitory activities against both the CVB3 and CV B6 at low concentrations(IC_(50)=1.42-7.15μM),whereas compounds 4d,7c,7e and 7g showed strong activity against CVB6(IC_(50)=2.91-3.77μM)together with low levels of activity against CVB3.Compound 7d exhibited stronger inhibitory activity against CVB3(IC_(50)=6.44μM)thaln CVB6(IC_(50)>8.29μM).The thioflavone derivatives 7a,7c,7d,7e,7f and 7g,represent a new class of lead compounds for the development of novel antiviral agents.
