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
The crystal structure of the title compound 1, C 22 H 30 BrNO 3, was determined by X ray analysis at 296(1)K. The crystal belongs to othorhombic system, space group P2 12 12 1 with a=9.842(5), b=12....The crystal structure of the title compound 1, C 22 H 30 BrNO 3, was determined by X ray analysis at 296(1)K. The crystal belongs to othorhombic system, space group P2 12 12 1 with a=9.842(5), b=12.510(5), c=17.763(6) , V=2187(3) 3, Z=4, M r=436.37, D x =1.33 g/cm 3, μ =18.79 cm 1 , F(000) =912 and the final R=0.047 and R w=0.053 for 1429 observed reflections with I≥3σ(I). Structure analysis reveals that the absolute configuration at C 14 of the acetal carbon of the title compound is S.展开更多
We previously showed that hydrogen sulfide(H2S)has a neuroprotective effect in the context of hypoxic ischemic brain injury in neonatal mice.However,the precise mechanism underlying the role of H2S in this situation r...We previously showed that hydrogen sulfide(H2S)has a neuroprotective effect in the context of hypoxic ischemic brain injury in neonatal mice.However,the precise mechanism underlying the role of H2S in this situation remains unclear.In this study,we used a neonatal mouse model of hypoxic ischemic brain injury and a lipopolysaccharide-stimulated BV2 cell model and found that treatment with L-cysteine,a H2S precursor,attenuated the cerebral infarction and cerebral atrophy induced by hypoxia and ischemia and increased the expression of miR-9-5p and cystathionineβsynthase(a major H2S synthetase in the brain)in the prefrontal cortex.We also found that an miR-9-5p inhibitor blocked the expression of cystathionineβsynthase in the prefrontal cortex in mice with brain injury caused by hypoxia and ischemia.Furthermore,miR-9-5p overexpression increased cystathionine-β-synthase and H2S expression in the injured prefrontal cortex of mice with hypoxic ischemic brain injury.L-cysteine decreased the expression of CXCL11,an miR-9-5p target gene,in the prefrontal cortex of the mouse model and in lipopolysaccharide-stimulated BV-2 cells and increased the levels of proinflammatory cytokines BNIP3,FSTL1,SOCS2 and SOCS5,while treatment with an miR-9-5p inhibitor reversed these changes.These findings suggest that H2S can reduce neuroinflammation in a neonatal mouse model of hypoxic ischemic brain injury through regulating the miR-9-5p/CXCL11 axis and restoringβ-synthase expression,thereby playing a role in reducing neuroinflammation in hypoxic ischemic brain injury.展开更多
以Web of Science数据库核心合集收录的1993篇文献为研究对象,采用CiteSpace可视化软件梳理Disinformation的研究动态和演进过程,使用5W2H分析法探讨Disinformation的潜在利益、传播动机等具体内涵。结合文献分析总结演化规律并对所预设...以Web of Science数据库核心合集收录的1993篇文献为研究对象,采用CiteSpace可视化软件梳理Disinformation的研究动态和演进过程,使用5W2H分析法探讨Disinformation的潜在利益、传播动机等具体内涵。结合文献分析总结演化规律并对所预设的7个问题进行系统性回答,就我国Disinformation的概念认知和信息迷雾治理提出建议。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The crystal structure of the title compound 1, C 22 H 30 BrNO 3, was determined by X ray analysis at 296(1)K. The crystal belongs to othorhombic system, space group P2 12 12 1 with a=9.842(5), b=12.510(5), c=17.763(6) , V=2187(3) 3, Z=4, M r=436.37, D x =1.33 g/cm 3, μ =18.79 cm 1 , F(000) =912 and the final R=0.047 and R w=0.053 for 1429 observed reflections with I≥3σ(I). Structure analysis reveals that the absolute configuration at C 14 of the acetal carbon of the title compound is S.
基金supported by the National Natural Science Foundation of China,Nos.82271327(to ZW),82072535(to ZW),81873768(to ZW),and 82001253(to TL).
文摘We previously showed that hydrogen sulfide(H2S)has a neuroprotective effect in the context of hypoxic ischemic brain injury in neonatal mice.However,the precise mechanism underlying the role of H2S in this situation remains unclear.In this study,we used a neonatal mouse model of hypoxic ischemic brain injury and a lipopolysaccharide-stimulated BV2 cell model and found that treatment with L-cysteine,a H2S precursor,attenuated the cerebral infarction and cerebral atrophy induced by hypoxia and ischemia and increased the expression of miR-9-5p and cystathionineβsynthase(a major H2S synthetase in the brain)in the prefrontal cortex.We also found that an miR-9-5p inhibitor blocked the expression of cystathionineβsynthase in the prefrontal cortex in mice with brain injury caused by hypoxia and ischemia.Furthermore,miR-9-5p overexpression increased cystathionine-β-synthase and H2S expression in the injured prefrontal cortex of mice with hypoxic ischemic brain injury.L-cysteine decreased the expression of CXCL11,an miR-9-5p target gene,in the prefrontal cortex of the mouse model and in lipopolysaccharide-stimulated BV-2 cells and increased the levels of proinflammatory cytokines BNIP3,FSTL1,SOCS2 and SOCS5,while treatment with an miR-9-5p inhibitor reversed these changes.These findings suggest that H2S can reduce neuroinflammation in a neonatal mouse model of hypoxic ischemic brain injury through regulating the miR-9-5p/CXCL11 axis and restoringβ-synthase expression,thereby playing a role in reducing neuroinflammation in hypoxic ischemic brain injury.
文摘以Web of Science数据库核心合集收录的1993篇文献为研究对象,采用CiteSpace可视化软件梳理Disinformation的研究动态和演进过程,使用5W2H分析法探讨Disinformation的潜在利益、传播动机等具体内涵。结合文献分析总结演化规律并对所预设的7个问题进行系统性回答,就我国Disinformation的概念认知和信息迷雾治理提出建议。
