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
目的:对比三维多回波恢复梯度回波(3D MERGE)、三维可变反转角快速自旋回波(3D SPACE STIR)序列在腰椎间盘突出症(LDH)检查中的应用效果。方法:选择2020年1月~2022年11月收治的135例LDH患者,回顾性分析患者临床和磁共振成像(MRI)资料,...目的:对比三维多回波恢复梯度回波(3D MERGE)、三维可变反转角快速自旋回波(3D SPACE STIR)序列在腰椎间盘突出症(LDH)检查中的应用效果。方法:选择2020年1月~2022年11月收治的135例LDH患者,回顾性分析患者临床和磁共振成像(MRI)资料,所有患者均接受常规MRI扫描及3D MERGE、3D SPACE STIR序列扫描,对比3D MERGE、3D SPACE STIR序列测量神经根直径的一致性,评价两种序列的图像质量参数[信噪比(SNR)、对比噪声比(CNR)]、图像清晰度评分。结果:3D MERGE和3D SPACE STIR序列测量的L3~S1神经根直径比较差异无统计学意义(P>0.05),且两组序列测量的L3、L4、L5和S1直径均显示出较高相关性(r=0.957,0.986,0.975,0.972,P<0.05);3D MERGE序列的SNR及CNR均高于3D SPACE STIR序列,神经根显示分级、图像清晰度评分优于3D SPACE STIR序列,差异有统计学意义(P<0.05)。结论:3D MERGE、3D SPACE STIR序列在LDH神经根直径测量中具有极高一致性,3D MERGE序列较3D SPACE STIR序列能够更清晰显示神经跟的解剖形态,图像质量更好。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.
文摘目的:对比三维多回波恢复梯度回波(3D MERGE)、三维可变反转角快速自旋回波(3D SPACE STIR)序列在腰椎间盘突出症(LDH)检查中的应用效果。方法:选择2020年1月~2022年11月收治的135例LDH患者,回顾性分析患者临床和磁共振成像(MRI)资料,所有患者均接受常规MRI扫描及3D MERGE、3D SPACE STIR序列扫描,对比3D MERGE、3D SPACE STIR序列测量神经根直径的一致性,评价两种序列的图像质量参数[信噪比(SNR)、对比噪声比(CNR)]、图像清晰度评分。结果:3D MERGE和3D SPACE STIR序列测量的L3~S1神经根直径比较差异无统计学意义(P>0.05),且两组序列测量的L3、L4、L5和S1直径均显示出较高相关性(r=0.957,0.986,0.975,0.972,P<0.05);3D MERGE序列的SNR及CNR均高于3D SPACE STIR序列,神经根显示分级、图像清晰度评分优于3D SPACE STIR序列,差异有统计学意义(P<0.05)。结论:3D MERGE、3D SPACE STIR序列在LDH神经根直径测量中具有极高一致性,3D MERGE序列较3D SPACE STIR序列能够更清晰显示神经跟的解剖形态,图像质量更好。