A novel method for achieving a copper（II）-catalyzed domino reaction for the construction of 2-aryl quinazolinones,without the addition of any ligand and additive,has been developed.The domino reaction achieved N-（a-substituted）benzylation,benzylic C–H amidation,and C–C（or C–H） bond cleavage.
PA_C subunit from avian influenza（H5N1） viral RNA polymerase was used in this work as a target in the screening for anti-influenza agents from licorice-derived compounds.As a result,18β-glycyrrhetinic acid was suggested to be PA_C ligand by flexible docking,and was then confirmed by relaxation-edited NMR.The result of ApG primer extension assay indicated that this PA_C ligand can inhibit the polymerase activity,and thus may potentially be valuable as anti-influenza lead compound.This work validated the possibility of screening polymerase inhibitors by using PA_C as a target,and provided a starting point for the further discovery of new anti-influenza drugs.
Lin LiSheng Hai ChangJun Feng XiangQian LiHuan Huan LiangYa Lin TangYing Fang Liu
Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, showed to strongly stabilize the intermolecular and intramolecular parallel stranded G-quadruplex structure, increasing melting temperature by 20 and 23℃, respectively. The binding mode was investigated by using NMR and molec- ular modelling methods. Four human cell lines （HL-60, BGC-823, Be1-7402 and KB） were taken to test the an- ti-proliferation effects of fangchinoline and the IC50 values were ranged from 16 to 32 μmol/L. These results showed that the fangchinoline or related moiety derivatives may represent a class of telomere-targeted agents as po- tential anti-cancer drugs.
