A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among the...A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among them,compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1 nmol/L to 0.92μmol/L.A preliminary SAR study of these derivatives was performed.展开更多
Cyclopropanedicarboxylic anhydride can be converted to 4-substituted (or 4-spiro-)3-oxabicyclo[3.1.0]hexan-2-one by addition of Grignard (or α,ω-di-Crignard) reagents in ether or tetrahydrofuran solution.
The stereoselective synthesis of 2-chloro-4-substituted-phenyl-5,5-dimethyl-1,3,2-dioxaphosphorinan-2-(thi)ones is described. Only single trans-isomers were obtained when 1-substituted-phenyl-2,2-dimethyl-1,3-propaned...The stereoselective synthesis of 2-chloro-4-substituted-phenyl-5,5-dimethyl-1,3,2-dioxaphosphorinan-2-(thi)ones is described. Only single trans-isomers were obtained when 1-substituted-phenyl-2,2-dimethyl-1,3-propanediols (1) reacted with POCl3. But the stereoselectivity of cyclization reaction between (1) and PSCl3 depended greatly upon the reaction condition. The configurational assignments and the ratio of cis-/trans- diastereoisomers of the products were performed on the basis of (HNMR)-H-1, (PNMR)-P-31 and IR spectra and confirmed by X-ray diffraction analyses.展开更多
Ten 4-substituted bicyclic phosphates were synthesized and their ^(13)C-NMR were also determined.A good relationship was observed between 4-^(13)C chemical shift and Taft σ_X induc- tive paramenters.Substituent effec...Ten 4-substituted bicyclic phosphates were synthesized and their ^(13)C-NMR were also determined.A good relationship was observed between 4-^(13)C chemical shift and Taft σ_X induc- tive paramenters.Substituent effects on ~3J_(P-C) coupling constant were studied.展开更多
Two new cadmium（II） and zinc（II） coordination polymers, {[Cd（btre）0.5- （mip）（H2O）2]·H2O}n （1） and [Zn（btre）（mip）]n （2）, were synthesized at room temperature condition and characterized by IR spe...Two new cadmium（II） and zinc（II） coordination polymers, {[Cd（btre）0.5- （mip）（H2O）2]·H2O}n （1） and [Zn（btre）（mip）]n （2）, were synthesized at room temperature condition and characterized by IR spectra, elemental analyses, single-crystal and powder X-ray diffractions （btre = 1,2-bis（1,2,4-triazol-4-yl）ethane, H2mip = 5-methyl-1,3-benzenedicarboxylic acid）. Complex 1 belongs to the triclinic system, P space group, with a = 8.9830（6）, b = 10.0579（6）, c = 10.2479（9） , α = 98.837（6）, β = 115.975（8）, γ = 106.370（6）°, V = 756.30（11） 3 and Z = 2; complex 2 crystallizes in monoclinic, space group P21/c, with a = 7.0332（3）, b = 14.9947（7）, c = 15.9689（7） ？, β = 97.1170（10）°, V = 1671.12（13） ？3 and Z = 4. Compounds 1 and 2 based on the same N/O-donor ligands show different structures. The one-dimensional chains of 1 are further linked by hydrogen bonding and π-π interactions to yield a three-dimensional supramolecular structure. The two-dimensional （6,3） networks of 2 are further extended into a 3D framework via π-π interactions. Thermal stabilities and luminescence of 1 and 2 were investigated.展开更多
It is a challenge to coordinate carrier-kinetics performance and the redox capacity of photogenerated charges synchronously at the atomic level for boosting photocatalytic activity.Herein,the atomic Ni was introduced ...It is a challenge to coordinate carrier-kinetics performance and the redox capacity of photogenerated charges synchronously at the atomic level for boosting photocatalytic activity.Herein,the atomic Ni was introduced into the lattice of hexagonal ZnIn_(2)S_(4) nanosheets(Ni/ZnIn_(2)S_(4))via directionalsubstituting Zn atom with the facile hydrothermal method.The electronic structure calculations indicate that the introduction of Ni atom effectively extracts more electrons and acts as active site for subsequent reduction reaction.Besides the optimized light absorption range,the elevation of Efand ECBendows Ni/ZnIn_(2)S_(4) photocatalyst with the increased electron concentration and the enhanced reduction ability for surface reaction.Moreover,ultrafast transient absorption spectroscopy,as well as a series of electrochemical tests,demonstrates that Ni/ZnIn_(2)S_(4) possesses 2.15 times longer lifetime of the excited charge carriers and an order of magnitude increase for carrier mobility and separation efficiency compared with pristine ZnIn_(2)S_(4).These efficient kinetics performances of charge carriers and enhanced redox capacity synergistically boost photocatalytic activity,in which a 3-times higher conversion efficiency of nitrobenzene reduction was achieved upon Ni/ZnIn_(2)S_(4).Our study not only provides in-depth insights into the effect of atomic directional-substitution on the kinetic behavior of photogenerated charges,but also opens an avenue to the synchronous optimization of redox capacity and carrier-kinetics performance for efficient solar energy conversion.展开更多
文摘A series of 1,4-substituted phthalazine derivatives were designed and synthesized.All the prepared compounds were screened for their cytotoxic activities against A549.HT-29 and MDA-MB-231 cell lines in vitro.Among them,compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1 nmol/L to 0.92μmol/L.A preliminary SAR study of these derivatives was performed.
文摘Cyclopropanedicarboxylic anhydride can be converted to 4-substituted (or 4-spiro-)3-oxabicyclo[3.1.0]hexan-2-one by addition of Grignard (or α,ω-di-Crignard) reagents in ether or tetrahydrofuran solution.
文摘The stereoselective synthesis of 2-chloro-4-substituted-phenyl-5,5-dimethyl-1,3,2-dioxaphosphorinan-2-(thi)ones is described. Only single trans-isomers were obtained when 1-substituted-phenyl-2,2-dimethyl-1,3-propanediols (1) reacted with POCl3. But the stereoselectivity of cyclization reaction between (1) and PSCl3 depended greatly upon the reaction condition. The configurational assignments and the ratio of cis-/trans- diastereoisomers of the products were performed on the basis of (HNMR)-H-1, (PNMR)-P-31 and IR spectra and confirmed by X-ray diffraction analyses.
基金Project Supported by National Sciences Foundation of China.
文摘Ten 4-substituted bicyclic phosphates were synthesized and their ^(13)C-NMR were also determined.A good relationship was observed between 4-^(13)C chemical shift and Taft σ_X induc- tive paramenters.Substituent effects on ~3J_(P-C) coupling constant were studied.
基金Supported by the Natural Science Foundation of Anhui Province(KJ2016A512)Key projects of Anhui Province University Outstanding Youth Talent Support Program(gxyqZD2016372)
文摘Two new cadmium（II） and zinc（II） coordination polymers, {[Cd（btre）0.5- （mip）（H2O）2]·H2O}n （1） and [Zn（btre）（mip）]n （2）, were synthesized at room temperature condition and characterized by IR spectra, elemental analyses, single-crystal and powder X-ray diffractions （btre = 1,2-bis（1,2,4-triazol-4-yl）ethane, H2mip = 5-methyl-1,3-benzenedicarboxylic acid）. Complex 1 belongs to the triclinic system, P space group, with a = 8.9830（6）, b = 10.0579（6）, c = 10.2479（9） , α = 98.837（6）, β = 115.975（8）, γ = 106.370（6）°, V = 756.30（11） 3 and Z = 2; complex 2 crystallizes in monoclinic, space group P21/c, with a = 7.0332（3）, b = 14.9947（7）, c = 15.9689（7） ？, β = 97.1170（10）°, V = 1671.12（13） ？3 and Z = 4. Compounds 1 and 2 based on the same N/O-donor ligands show different structures. The one-dimensional chains of 1 are further linked by hydrogen bonding and π-π interactions to yield a three-dimensional supramolecular structure. The two-dimensional （6,3） networks of 2 are further extended into a 3D framework via π-π interactions. Thermal stabilities and luminescence of 1 and 2 were investigated.
基金the National Natural Science Foundation of China (22209091)the Natural Science Foundation of Shandong Province (ZR2020QB057)+1 种基金the Key Program of National Natural Science Foundation of China (22133006)the Yankuang Group 2019 Science and Technology Program (YKKJ2019AJ05JG-R60)。
文摘It is a challenge to coordinate carrier-kinetics performance and the redox capacity of photogenerated charges synchronously at the atomic level for boosting photocatalytic activity.Herein,the atomic Ni was introduced into the lattice of hexagonal ZnIn_(2)S_(4) nanosheets(Ni/ZnIn_(2)S_(4))via directionalsubstituting Zn atom with the facile hydrothermal method.The electronic structure calculations indicate that the introduction of Ni atom effectively extracts more electrons and acts as active site for subsequent reduction reaction.Besides the optimized light absorption range,the elevation of Efand ECBendows Ni/ZnIn_(2)S_(4) photocatalyst with the increased electron concentration and the enhanced reduction ability for surface reaction.Moreover,ultrafast transient absorption spectroscopy,as well as a series of electrochemical tests,demonstrates that Ni/ZnIn_(2)S_(4) possesses 2.15 times longer lifetime of the excited charge carriers and an order of magnitude increase for carrier mobility and separation efficiency compared with pristine ZnIn_(2)S_(4).These efficient kinetics performances of charge carriers and enhanced redox capacity synergistically boost photocatalytic activity,in which a 3-times higher conversion efficiency of nitrobenzene reduction was achieved upon Ni/ZnIn_(2)S_(4).Our study not only provides in-depth insights into the effect of atomic directional-substitution on the kinetic behavior of photogenerated charges,but also opens an avenue to the synchronous optimization of redox capacity and carrier-kinetics performance for efficient solar energy conversion.
