The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was establishe...The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR and mass spectroscopy. These new compounds were tested for their antiproliferative activities on seven representative human tumoral cell lines (Huh7 D12, Caco2, MDA-MB231, MDA-MB468, HCT116, PC3 and MCF7) and also on fibroblasts. Among them, only the compounds 6c showed micromolar cytotoxic activity on tumor cell lines (1.8 50 50 > 25 μM). Finally, in silico ADMET studies ware performed to investigate the possibility of using of the identified compound 6c as potential anti-tumor compound.展开更多
In this paper, we report the tandem Michael addition-elimination reactions of chiral 5-alkoxy-3,4-dihalo-2（5H）-furanones with DMF by the catalyst of metal sodium. The optically pure 5-（S）-alkoxy-4-N,N-dimethyl-3-h...In this paper, we report the tandem Michael addition-elimination reactions of chiral 5-alkoxy-3,4-dihalo-2（5H）-furanones with DMF by the catalyst of metal sodium. The optically pure 5-（S）-alkoxy-4-N,N-dimethyl-3-halo-2（5H）-furanones 6a6d were identified on the basis of their analytical data, such as [α]20D , UV, IR, 1H NMR, 13C NMR, MS and elemental analysis.展开更多
文摘The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR and mass spectroscopy. These new compounds were tested for their antiproliferative activities on seven representative human tumoral cell lines (Huh7 D12, Caco2, MDA-MB231, MDA-MB468, HCT116, PC3 and MCF7) and also on fibroblasts. Among them, only the compounds 6c showed micromolar cytotoxic activity on tumor cell lines (1.8 50 50 > 25 μM). Finally, in silico ADMET studies ware performed to investigate the possibility of using of the identified compound 6c as potential anti-tumor compound.
文摘In this paper, we report the tandem Michael addition-elimination reactions of chiral 5-alkoxy-3,4-dihalo-2（5H）-furanones with DMF by the catalyst of metal sodium. The optically pure 5-（S）-alkoxy-4-N,N-dimethyl-3-halo-2（5H）-furanones 6a6d were identified on the basis of their analytical data, such as [α]20D , UV, IR, 1H NMR, 13C NMR, MS and elemental analysis.
