The title compound 4-（4,6-dimethoxylpyrimidin-2-yl）-3-thiourea carboxylic acid methyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in eth...The title compound 4-（4,6-dimethoxylpyrimidin-2-yl）-3-thiourea carboxylic acid methyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in ethyl acetate. Single crystals suitable for X-ray measurement were obtained by recrystallization with the solvent of dimethyl formamide at the room temperature. The structure was characterized by elemental analysis and IR and determined by X-ray diffraction analysis＇ Crystallographic data： C9H12N4O4S, Mr = 272.29, monoclinic, space group C2/m with a = 1.6672（3）, b = 0.66383（12）, c = 1.1617（2） nm, β = 109.275（2）°, V = 1.2136（4） nm^3, Dc = 1.490 g/cm^3,μ = 0.281 mm^-1, F（000） = 568, Z = 4, R1 = 0.0341and wR2 = 0.1042.展开更多
4-（4,6-Dimethoxyl-pyrimidin-2-yl）-3-thiourea carboxylic acid ethyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in ethyl acetate. Single ...4-（4,6-Dimethoxyl-pyrimidin-2-yl）-3-thiourea carboxylic acid ethyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in ethyl acetate. Single crystals suitable for X-ray measurement were obtained by recrystallization with the solvent of dimethyl formamide at room temperature. The crystal structure was determined by X-ray diffraction analysis. Crystallographic data： C10H14N4O4S, M, = 286.31, monoclinic, space group C2/c with a = 2.5309（3）, b = 0.67682（6）, c = 1.74237（19） nm, β = 114.744（3）°, V= 2.7106（5） nm3, Dc = 1.403 g/cm3, p = 0.225 mm-1, F（000） = 1200, Z= 8, R= 0.0514 and wR= 0.1529.展开更多
目的探讨骨代谢相关指标与围绝经期骨质疏松病人发生骨质疏松相关性骨折的关系。方法选取2015年10月至2018年5月濮阳市第三人民医院收治的44例围绝经期骨质疏松且发生骨折的病人作为病例组、80例围绝经期骨质疏松但是未发生骨折的病人...目的探讨骨代谢相关指标与围绝经期骨质疏松病人发生骨质疏松相关性骨折的关系。方法选取2015年10月至2018年5月濮阳市第三人民医院收治的44例围绝经期骨质疏松且发生骨折的病人作为病例组、80例围绝经期骨质疏松但是未发生骨折的病人作为对照组;调查对比两组的一般资料、血清Ⅰ型前胶原氨基端前肽(N-terminal propeptide of type procolla‐gen,P1NP)、Ⅰ型胶原羧基端肽β特殊序列(Special sequence ofβ-carboxyl terminal peptide of typeⅠcollagen,β-CTX)、骨钙素N端中分子(Osteocalcin N-terminus molecule,N-MID)、25-羟基维生素D[25-hydroxyvitamin D,25-(OH)VitD]的水平;采用logistic多因素分析上述指标与围绝经期骨质疏松且发生骨折的关系。结果病例组和对照组的年龄、体质量指数(BMI)、骨折病史、是否参与体育锻炼、每天的日照时间、吸烟、饮酒、高血压、血脂异常均差异无统计学意义(P>0.05);病例组的骨密度为(0.48±0.07)g/cm^(2),明显低于对照组的(0.56±0.08)g/cm^(2)(P<0.001),病例组的糖尿病合并率为25%,高于对照组的5%(P<0.05);病例组病人血清P1NP、β-CTX的水平分别为(64.81±10.44)μg/L、(0.68±0.07)μg/L,明显高于对照组的(52.07±8.95)μg/L、(0.60±0.08)μg/L(P<0.001),病例组25-(OH)VitD水平为(21.84±2.40)μg/L,明显低于对照组的(25.40±3.12)μg/L(P<0.001);经logistic回归分析,血清P1NP、β-CTX的水平升高、25-(OH)VitD水平降低、骨密度降低、合并糖尿病是围绝经期骨质疏松发生骨折的独立危险因素(P<0.05)。结论血清P1NP、β-CTX的水平升高、25-(OH)VitD水平降低会增大围绝经期骨质疏松发生骨折的风险。展开更多
Vitamin B12 was applied as catalyst for the one-pot three-component synthesis of 3,4,5-trisubstituted furan-2（5H）-ones from the condensation between aldehydes, amines and dialkylacetylendicarboxylates at ambient tem...Vitamin B12 was applied as catalyst for the one-pot three-component synthesis of 3,4,5-trisubstituted furan-2（5H）-ones from the condensation between aldehydes, amines and dialkylacetylendicarboxylates at ambient temperature in Et OH. In addition, N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates were synthesised using mentioned catalyst at ambient temperature in Et OH from condensation between formaldehyde, amines, and dialkylacetylenedicarboxylates. This methodology has number of advantages such as： use of green and nonhazardous catalyst, clean work up, short reaction times,high yields and no need to column chromatography.展开更多
Objective： To study apoptotic effects of synthetic retinoic acid 6-[3-（1-adamantyl）-4-hydroxyphenyl]-2-naphthalene carboxylic acid（AHPN） on human skin malignant melanoma A375 cells in comparison with the natural ...Objective： To study apoptotic effects of synthetic retinoic acid 6-[3-（1-adamantyl）-4-hydroxyphenyl]-2-naphthalene carboxylic acid（AHPN） on human skin malignant melanoma A375 cells in comparison with the natural ligand all-trans-retinoic acid（ATRA） in vitro and the mechanisms related to the actions of AHPN. Methods：MTT assay was used to determine the anti-proliferative effects of AHPN and ATRA on A375 cells. Flow cytometry was performed to investigate the influence of AHPN and ATRA on cell cycle and cell apoptosis. In addition, transfection and luciferase activity assays were employed to explore the mechanisms of how AHPN executes its proapoptotic function. Results：Firstly, AHPN promoted apoptosis and GI arrest in A375 cells compared with ATRA. Secondly, the activity of NF-K B in A375 cells treated with AHPN increased 2-3 times compared with solvent DMSO treatment. Conclusion：AHPN, in comparison with ATRA, is a more effective alternative for therapy of malignant melanoma. The potentially proapoptotic function of AHPN requires activation of NF-K B.展开更多
基金This work was supported by the National Natural Science Foundation of China (20571060) and Education Committee of Shaan Xi Province (05JK294)
文摘The title compound 4-（4,6-dimethoxylpyrimidin-2-yl）-3-thiourea carboxylic acid methyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in ethyl acetate. Single crystals suitable for X-ray measurement were obtained by recrystallization with the solvent of dimethyl formamide at the room temperature. The structure was characterized by elemental analysis and IR and determined by X-ray diffraction analysis＇ Crystallographic data： C9H12N4O4S, Mr = 272.29, monoclinic, space group C2/m with a = 1.6672（3）, b = 0.66383（12）, c = 1.1617（2） nm, β = 109.275（2）°, V = 1.2136（4） nm^3, Dc = 1.490 g/cm^3,μ = 0.281 mm^-1, F（000） = 568, Z = 4, R1 = 0.0341and wR2 = 0.1042.
基金supported by the National Natural Science Foundation of China (20571060)Natural Science Foundation of Shaanxi Province (2007B08)Education Committee of Shaanxi Province (05JK294)
文摘4-（4,6-Dimethoxyl-pyrimidin-2-yl）-3-thiourea carboxylic acid ethyl ester was synthesized by the reaction of 2-amino-4,6-dimethoxyl pyrimidine, potassium thiocyanate and methyl chloroformate in ethyl acetate. Single crystals suitable for X-ray measurement were obtained by recrystallization with the solvent of dimethyl formamide at room temperature. The crystal structure was determined by X-ray diffraction analysis. Crystallographic data： C10H14N4O4S, M, = 286.31, monoclinic, space group C2/c with a = 2.5309（3）, b = 0.67682（6）, c = 1.74237（19） nm, β = 114.744（3）°, V= 2.7106（5） nm3, Dc = 1.403 g/cm3, p = 0.225 mm-1, F（000） = 1200, Z= 8, R= 0.0514 and wR= 0.1529.
文摘目的探讨骨代谢相关指标与围绝经期骨质疏松病人发生骨质疏松相关性骨折的关系。方法选取2015年10月至2018年5月濮阳市第三人民医院收治的44例围绝经期骨质疏松且发生骨折的病人作为病例组、80例围绝经期骨质疏松但是未发生骨折的病人作为对照组;调查对比两组的一般资料、血清Ⅰ型前胶原氨基端前肽(N-terminal propeptide of type procolla‐gen,P1NP)、Ⅰ型胶原羧基端肽β特殊序列(Special sequence ofβ-carboxyl terminal peptide of typeⅠcollagen,β-CTX)、骨钙素N端中分子(Osteocalcin N-terminus molecule,N-MID)、25-羟基维生素D[25-hydroxyvitamin D,25-(OH)VitD]的水平;采用logistic多因素分析上述指标与围绝经期骨质疏松且发生骨折的关系。结果病例组和对照组的年龄、体质量指数(BMI)、骨折病史、是否参与体育锻炼、每天的日照时间、吸烟、饮酒、高血压、血脂异常均差异无统计学意义(P>0.05);病例组的骨密度为(0.48±0.07)g/cm^(2),明显低于对照组的(0.56±0.08)g/cm^(2)(P<0.001),病例组的糖尿病合并率为25%,高于对照组的5%(P<0.05);病例组病人血清P1NP、β-CTX的水平分别为(64.81±10.44)μg/L、(0.68±0.07)μg/L,明显高于对照组的(52.07±8.95)μg/L、(0.60±0.08)μg/L(P<0.001),病例组25-(OH)VitD水平为(21.84±2.40)μg/L,明显低于对照组的(25.40±3.12)μg/L(P<0.001);经logistic回归分析,血清P1NP、β-CTX的水平升高、25-(OH)VitD水平降低、骨密度降低、合并糖尿病是围绝经期骨质疏松发生骨折的独立危险因素(P<0.05)。结论血清P1NP、β-CTX的水平升高、25-(OH)VitD水平降低会增大围绝经期骨质疏松发生骨折的风险。
基金financial support from the Research Council of the University of Sistan and Baluchestan,Zahedan, Iran
文摘Vitamin B12 was applied as catalyst for the one-pot three-component synthesis of 3,4,5-trisubstituted furan-2（5H）-ones from the condensation between aldehydes, amines and dialkylacetylendicarboxylates at ambient temperature in Et OH. In addition, N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates were synthesised using mentioned catalyst at ambient temperature in Et OH from condensation between formaldehyde, amines, and dialkylacetylenedicarboxylates. This methodology has number of advantages such as： use of green and nonhazardous catalyst, clean work up, short reaction times,high yields and no need to column chromatography.
文摘Objective： To study apoptotic effects of synthetic retinoic acid 6-[3-（1-adamantyl）-4-hydroxyphenyl]-2-naphthalene carboxylic acid（AHPN） on human skin malignant melanoma A375 cells in comparison with the natural ligand all-trans-retinoic acid（ATRA） in vitro and the mechanisms related to the actions of AHPN. Methods：MTT assay was used to determine the anti-proliferative effects of AHPN and ATRA on A375 cells. Flow cytometry was performed to investigate the influence of AHPN and ATRA on cell cycle and cell apoptosis. In addition, transfection and luciferase activity assays were employed to explore the mechanisms of how AHPN executes its proapoptotic function. Results：Firstly, AHPN promoted apoptosis and GI arrest in A375 cells compared with ATRA. Secondly, the activity of NF-K B in A375 cells treated with AHPN increased 2-3 times compared with solvent DMSO treatment. Conclusion：AHPN, in comparison with ATRA, is a more effective alternative for therapy of malignant melanoma. The potentially proapoptotic function of AHPN requires activation of NF-K B.
