Twenty five samples of 4,4'-disubstituted stilbene derivatives were synthesized, and their UV absorption max wavelengths were determined in over 10 kinds of solvents including cyclohexane, ether, chloroform, aceto...Twenty five samples of 4,4'-disubstituted stilbene derivatives were synthesized, and their UV absorption max wavelengths were determined in over 10 kinds of solvents including cyclohexane, ether, chloroform, acetonitrile and ethanol, in which 242 experimental data were recorded. The effects of substituents and solvents on the energy of their UV absorption max wavelengths were discussed. The research results showed: the energy of UV absorption max wavelengths of 4,4'-disubstituted stilbenes was mainly affected by their intramolecular structure (substituent effect) in a given solvent, that is, the energy is dominated by both of excited-state substituent parameter o-~c and polar substituent constant crp. While their energy was dominated by the substituent effect and solvent effect in different kinds of solvents. An equation quantifying the energy of UV absorption max wavelengths of 4,4'-disubstituted stilbenes was developed. In addition, it is found that the n-octanol/water partition coefficient (logP) is more effective than the solvatochromic dye (ET(30)) in scaling the solvent effect. The equation employed the parameter logP has a better correlation and more specific physical meaning. Further, the energies of UV absorption max wavelengths of some reported compounds were predicted by the obtained equation, which are in agreement with their experimental values.展开更多
Two new resveratrol analougues,t-butyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy i-butyrate and ethyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy n-butyrate,are synthesized from 3,4,5-trimethoxybenzaldehyde an...Two new resveratrol analougues,t-butyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy i-butyrate and ethyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy n-butyrate,are synthesized from 3,4,5-trimethoxybenzaldehyde and p-nitrotoluene via mutil-steps including condensation,catalytic reduction,diazotization,hydrolyzation,nucleophilic substitution.The effect of the new compounds on HL-60 and A549 cell proliferation are tested by MTT.The results show that the two new compounds exhibite the activities of anti-tumor proliferation.展开更多
Fatty acid synthase （FAS） attracts more and more attention recently as a potential target for metabolic syndrome,such as cancer, obesity, diabetes and cerebrovascular disease. FAS inhibitors are widely existed in pl...Fatty acid synthase （FAS） attracts more and more attention recently as a potential target for metabolic syndrome,such as cancer, obesity, diabetes and cerebrovascular disease. FAS inhibitors are widely existed in plants, consisting of diversiform compounds. These inhibitors exist not only in herbs also in many plant foods, such as teas, allium vegetables and some fruits. These effective components include gallated catechins, theaflavins,flavonoids, condensed and hydrolysable tannins, thioethers,pentacyclic triterpenes, stilbene derivatives, etc, and they target at the different domains of FAS, showing different inhibitory mechanisms. Interestingly, these FAS inhibitor-contained herbs and plant foods and their effective components are commonly related to the prevention of metabolic syndromes including fatreducing and depression of cancer. From biochemical angle,FAS can control the balance between energy provision and fat production. Some studies have shown that the effects of those effective components in plants on metabolic syndromes are mediated by inhibiting FAS. This suggests that FAS plays a critical role in the regulation of energy metabolism, and the FAS inhibitors from plants have significant potential application value in the treatment and prevention of metabolic syndromes.展开更多
以6-氟-4-氯喹唑啉与反式-4-(2-芳基乙烯基)苯胺类化合物为原料,经胺化反应,合成了4-[4-((E-)3,4,5-三甲氧基苯乙烯基)]苯氨基-6-氟喹唑啉等六种新型4-芳氨基-6-氟喹唑啉类衍生物,收率55%～76%,其结构利用1 H NMR,IR和元素分析进行确证....以6-氟-4-氯喹唑啉与反式-4-(2-芳基乙烯基)苯胺类化合物为原料,经胺化反应,合成了4-[4-((E-)3,4,5-三甲氧基苯乙烯基)]苯氨基-6-氟喹唑啉等六种新型4-芳氨基-6-氟喹唑啉类衍生物,收率55%～76%,其结构利用1 H NMR,IR和元素分析进行确证.1 H NMR分析表明,化合物在δ9.74～9.79出现的单峰为4位的—NH所产生;IR谱图中,化合物在3 618～3 278cm-1出现一个吸收峰,同样证明了目标化合物的生成.展开更多
基金financially supported by the National Natural Science Foundation of China (21072053 & 20772028) the Scientific Research Fund of Hunan Provincial Education Department (10K025)
文摘Twenty five samples of 4,4'-disubstituted stilbene derivatives were synthesized, and their UV absorption max wavelengths were determined in over 10 kinds of solvents including cyclohexane, ether, chloroform, acetonitrile and ethanol, in which 242 experimental data were recorded. The effects of substituents and solvents on the energy of their UV absorption max wavelengths were discussed. The research results showed: the energy of UV absorption max wavelengths of 4,4'-disubstituted stilbenes was mainly affected by their intramolecular structure (substituent effect) in a given solvent, that is, the energy is dominated by both of excited-state substituent parameter o-~c and polar substituent constant crp. While their energy was dominated by the substituent effect and solvent effect in different kinds of solvents. An equation quantifying the energy of UV absorption max wavelengths of 4,4'-disubstituted stilbenes was developed. In addition, it is found that the n-octanol/water partition coefficient (logP) is more effective than the solvatochromic dye (ET(30)) in scaling the solvent effect. The equation employed the parameter logP has a better correlation and more specific physical meaning. Further, the energies of UV absorption max wavelengths of some reported compounds were predicted by the obtained equation, which are in agreement with their experimental values.
文摘Two new resveratrol analougues,t-butyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy i-butyrate and ethyl 4-[(E)-2-(3,4,5-trimethoxyphenyl)vinyl]phenoxy n-butyrate,are synthesized from 3,4,5-trimethoxybenzaldehyde and p-nitrotoluene via mutil-steps including condensation,catalytic reduction,diazotization,hydrolyzation,nucleophilic substitution.The effect of the new compounds on HL-60 and A549 cell proliferation are tested by MTT.The results show that the two new compounds exhibite the activities of anti-tumor proliferation.
文摘Fatty acid synthase （FAS） attracts more and more attention recently as a potential target for metabolic syndrome,such as cancer, obesity, diabetes and cerebrovascular disease. FAS inhibitors are widely existed in plants, consisting of diversiform compounds. These inhibitors exist not only in herbs also in many plant foods, such as teas, allium vegetables and some fruits. These effective components include gallated catechins, theaflavins,flavonoids, condensed and hydrolysable tannins, thioethers,pentacyclic triterpenes, stilbene derivatives, etc, and they target at the different domains of FAS, showing different inhibitory mechanisms. Interestingly, these FAS inhibitor-contained herbs and plant foods and their effective components are commonly related to the prevention of metabolic syndromes including fatreducing and depression of cancer. From biochemical angle,FAS can control the balance between energy provision and fat production. Some studies have shown that the effects of those effective components in plants on metabolic syndromes are mediated by inhibiting FAS. This suggests that FAS plays a critical role in the regulation of energy metabolism, and the FAS inhibitors from plants have significant potential application value in the treatment and prevention of metabolic syndromes.
文摘以6-氟-4-氯喹唑啉与反式-4-(2-芳基乙烯基)苯胺类化合物为原料,经胺化反应,合成了4-[4-((E-)3,4,5-三甲氧基苯乙烯基)]苯氨基-6-氟喹唑啉等六种新型4-芳氨基-6-氟喹唑啉类衍生物,收率55%～76%,其结构利用1 H NMR,IR和元素分析进行确证.1 H NMR分析表明,化合物在δ9.74～9.79出现的单峰为4位的—NH所产生;IR谱图中,化合物在3 618～3 278cm-1出现一个吸收峰,同样证明了目标化合物的生成.
