A 1 -octadecanol (OD)/1,3:2,4-di-(3,4-dimethyl) benzylidene sorbitol (DMDBS)/expander graphite (EG) composite was prepared as a form-stable phase change material (PCM) by vacuum melting method. The results of field em...A 1 -octadecanol (OD)/1,3:2,4-di-(3,4-dimethyl) benzylidene sorbitol (DMDBS)/expander graphite (EG) composite was prepared as a form-stable phase change material (PCM) by vacuum melting method. The results of field emission-scanning electron microscopy (FE-SEM) showed that 1 -octadecanol was restricted in the three-dimensional network formed by DMDBS and the honeycomb network formed by EG. X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) results showed that no chemical reaction occurred among the components of composite PCM in the preparation process. The gel-to-sol transition temperature of the composite PCMs containing DMDBS was much higher than the melting point of pure 1-octadecanol. The improvements in preventing leakage and thermal stability limits were mainly attributed to the synergistic effect of the three-dimensional network formed by DMDBS and the honeycomb network formed by EG. Differential scanning calorimeter (DSC) was used to determine the latent heat and phase change temperature of the composite PCMs. During melting and freezing process the latent heat values of the PCM with the composition of 91% OD/3% DMDBS/6% EG were 214.9 and 185.9 kJ kg'1, respectively. Its degree of supercooling was only 0.1 °C. Thermal constant analyzer results showed that its thermal conductivity (k) changed up to roughly 10 times over that of OD/DMDBS matrix.展开更多
Estrogen receptor(ER)αis expressed in a subset of patient-derived acute myeloid leukemia(AML)cells,whereas Akt is predominantly expressed in most types of AML.Targeting AML with dual inhibitors is a novel approach to...Estrogen receptor(ER)αis expressed in a subset of patient-derived acute myeloid leukemia(AML)cells,whereas Akt is predominantly expressed in most types of AML.Targeting AML with dual inhibitors is a novel approach to combat the disease.Herein,we examined a novel small molecule,3-(4-isopropyl)benzylidene-8-ethoxy,6-methyl,chroman-4-one(SBL-060),capable of targeting AML cells by inhibiting ERαand Akt kinase.The chemical properties of SBL-060 were identified by proton nuclear magnetic resonance(^(1)H-NMR),^(13)C-NMR,and mass spectroscopy.In silico docking was performed using an automated protocol with AutoDock-VINA.THP-1 and HL-60 cell lines were differentiated using phorbol 12-myristate 13-acetate.ERαinhibition was assessed using ELISA.The MTT assay assessed cell viability.Flow cytometry was performed for cell cycle,apoptosis,and p-Akt analyses.Chemical analysis identified the compound as 3-(4-isopropyl)benzylidene-8-ethoxy,6-methyl,chroman-4-one,which showed high binding efficacy toward ER,with aΔG_(binding) score of−7.4 kcal/mol.SBL-060 inhibited ERα,exhibiting IC50 values of 448 and 374.3 nM in THP-1 and HL-60 cells,respectively.Regarding inhibited cell proliferation,GI50 values of SBL-060 were 244.1 and 189.9 nM for THP-1 and HL-60 cells,respectively.In addition,a dose-dependent increase in sub G_(0)/G_(1) phase cell cycle arrest and total apoptosis was observed after treatment with SBL-060 in both cell types.SBL-060 also dose-dependently increased the p-Akt-positive populations in both THP-1 and HL-60 cells.Our results indicate that SBL-060 has excellent efficacy against differentiated AML cell types by inhibiting ER and Akt kinase,warranting further preclinical evaluations.展开更多
A new method for the cleavage of carbohydrate benzylidene acetal has been developed using Ceric (YV) ammonium nitrate (CAN) [(NH4)2Ce(NO3)6] in CH3CN-H2O (10/1, v/v).
A versatile and environmentally friendly method for α,α’-bis(substituted ben-zylidene) cycloalkanones has been developed using a heterogeneous catalysis technology. We have synthesized a series of the α,α’-bis(s...A versatile and environmentally friendly method for α,α’-bis(substituted ben-zylidene) cycloalkanones has been developed using a heterogeneous catalysis technology. We have synthesized a series of the α,α’-bis(substituted benzylidene) cycloalkanones, a biologically important class of compounds, via the cross aldol condensation between arylaldehydes and cycloketones using sodium-modified fluorapatite (Na/FAP) as a highly efficient solid catalyst under conventional heating in aqueous media and solventless conditions under microwave. Catalyst reuse, ease of separation of the pure product, and high yields are some of the unique features of this process. Shorter reaction times (4 - 7 min) and higher yields (80% - 94%) were achieved under microwave irradiation conditions.展开更多
A green and highly efficient strategy for the preparation of bridged spirocyclic compounds via visible-light-induced cyclization of 2-(2-(arylethynyl)benzylidene)malononitrile derivatives with 2,6-di(tert-butyl)-4-met...A green and highly efficient strategy for the preparation of bridged spirocyclic compounds via visible-light-induced cyclization of 2-(2-(arylethynyl)benzylidene)malononitrile derivatives with 2,6-di(tert-butyl)-4-methylphenol(BHT)at room temperature was developed.The photoinduced radical reactions generated the corresponding products in good yields under simple and mild reaction conditions.展开更多
An unexpected synthesis of an α, β, γ,δ-unsaturated ketone, which embodies a new type of oxy-carbon cyclic structure, was achieved, while we tried to construct the taxane CB-ring system. Also, a series of abnormal...An unexpected synthesis of an α, β, γ,δ-unsaturated ketone, which embodies a new type of oxy-carbon cyclic structure, was achieved, while we tried to construct the taxane CB-ring system. Also, a series of abnormal reaction phenomena was found to be related to the formation and reaction of seven membered cyclic benzylidene acetal.展开更多
In this work we synthesized new derivatives from Phenyl Hydrazine and series of different Aldehydes (derivatives of benzylidenes). The synthesized compounds contain different aromatic Aldehydes which attached by Benze...In this work we synthesized new derivatives from Phenyl Hydrazine and series of different Aldehydes (derivatives of benzylidenes). The synthesized compounds contain different aromatic Aldehydes which attached by Benzene ring via Hydrazine moiety in glacial acetic acid. These derivatives were characterized by TLC, melting points, Infrared Red, Proton Nuclear Magnetic Resonance, Carbon Thirteen Nuclear Magnetic Resonance and Mass Spectroscopy. Finally, these synthesized derivatives were tested for antiproliferative activity against multiple normal and cancerous cell lines, HepG2 (Liver cancer) and MCF-7 (Breast cancer) cell lines were used for cytotoxic assay.展开更多
In this work, some new oxadiazole derivatives have been prepared, by reacting phenyl hydrazine and acetic anhydride together, which furnished 2,4-dimethyl-4-phenyloxadiazole. This product was reacted with a series of ...In this work, some new oxadiazole derivatives have been prepared, by reacting phenyl hydrazine and acetic anhydride together, which furnished 2,4-dimethyl-4-phenyloxadiazole. This product was reacted with a series of aromatic aldehydes, to obtain a series of oxadiazole derivatives. These derivatives were characterized by TLC, melting points, infrared red, proton nuclear magnetic resonance, carbon thirteen nuclear magnetic resonance and mass spectroscopy. Finally, these synthetized derivatives were tested for antiproliferative activity by two different cell lines. MCF-7 (Breast cancer cell line) and HepG2 (Liver cancer cell line) were used to assess the antiproliferative activity of the prepared compounds.展开更多
A versatile synthetic approach toward a series of benzothiazepines with medicinal potential (for example, compound <strong>1</strong>) that allows incorporation of structural variation at the three aromati...A versatile synthetic approach toward a series of benzothiazepines with medicinal potential (for example, compound <strong>1</strong>) that allows incorporation of structural variation at the three aromatic regions of the structure, and at the sulfur atom, was developed. Knoevenagel condensation of indan-1,3-diones with benzaldehydes, yielded 2-benzylidineindan-1,3-diones, which undewent thio-Michael addition and intramolecular imine formation upon reaction with 2-aminothiophenols, to produce the target benzothiazepines. Use of indan-1,3-diones, benzaldehydes or 2-aminothiophenols bearing further substitution enabled production of novel 5,11-dihydro-12H-benzo[b]indeno [1,2-e][1,4]thiazepin-12-one analogs <strong>1</strong> - <strong>14</strong>, including compounds bearing substitution at novel positions within the scaffold.展开更多
A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing a...A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing ability to 15 metal ions was investigated.Weak emission from TBB could be efficiently increased by trace Hg^2+,through coordination reaction between TBB and Hg^2+ with"turn on"character.The fluorescence intensity of TBB/Hg^2+([TBB]=3.0×10^–6 mol/L,[Hg2+]=1.3×10^–4 mol/L)was 7.5 times higher than that of TBB.This TBB sensor exhibited high selectivity for Hg^2+ and other metal ions did not interfere in this determination.The limit of detection was 0.566μmol/L(S/N=3).The experimental results showed that this TBB sensor could sensitively respond to Hg^2+ within concentration range(from 5×10–6 mol/L to 1.3×10^–4 mol/L).展开更多
Propyl O-(α-L-rhamncpyranosyl)-(1→3)-[2,4-di-O-(2s-methylbutyryl)-α-L-rham-nopyranosyl]-(1→2)-(3-O-acetyl-β-D-glucopyranosyl)-(1→2)-β-D-fucopyranoside (1), the tetrasac-charide moiety of Tricolorin A, was synth...Propyl O-(α-L-rhamncpyranosyl)-(1→3)-[2,4-di-O-(2s-methylbutyryl)-α-L-rham-nopyranosyl]-(1→2)-(3-O-acetyl-β-D-glucopyranosyl)-(1→2)-β-D-fucopyranoside (1), the tetrasac-charide moiety of Tricolorin A, was synthesized in total 23 steps with a longest linear sequence of 10 steps, and overall yield of 3.7% from D-Glucose. The isomerization of the dioxolane-type berzyli-dene in the presence of NIS/AgOTf was observed. Tetrasaccharide 1 exhibited no activity against the cultured P388 cell as Tricolorin A did.展开更多
基金Funded by Science and Technology Support Program of Hubei Province of China(No.2015BAA111)
文摘A 1 -octadecanol (OD)/1,3:2,4-di-(3,4-dimethyl) benzylidene sorbitol (DMDBS)/expander graphite (EG) composite was prepared as a form-stable phase change material (PCM) by vacuum melting method. The results of field emission-scanning electron microscopy (FE-SEM) showed that 1 -octadecanol was restricted in the three-dimensional network formed by DMDBS and the honeycomb network formed by EG. X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) results showed that no chemical reaction occurred among the components of composite PCM in the preparation process. The gel-to-sol transition temperature of the composite PCMs containing DMDBS was much higher than the melting point of pure 1-octadecanol. The improvements in preventing leakage and thermal stability limits were mainly attributed to the synergistic effect of the three-dimensional network formed by DMDBS and the honeycomb network formed by EG. Differential scanning calorimeter (DSC) was used to determine the latent heat and phase change temperature of the composite PCMs. During melting and freezing process the latent heat values of the PCM with the composition of 91% OD/3% DMDBS/6% EG were 214.9 and 185.9 kJ kg'1, respectively. Its degree of supercooling was only 0.1 °C. Thermal constant analyzer results showed that its thermal conductivity (k) changed up to roughly 10 times over that of OD/DMDBS matrix.
文摘Estrogen receptor(ER)αis expressed in a subset of patient-derived acute myeloid leukemia(AML)cells,whereas Akt is predominantly expressed in most types of AML.Targeting AML with dual inhibitors is a novel approach to combat the disease.Herein,we examined a novel small molecule,3-(4-isopropyl)benzylidene-8-ethoxy,6-methyl,chroman-4-one(SBL-060),capable of targeting AML cells by inhibiting ERαand Akt kinase.The chemical properties of SBL-060 were identified by proton nuclear magnetic resonance(^(1)H-NMR),^(13)C-NMR,and mass spectroscopy.In silico docking was performed using an automated protocol with AutoDock-VINA.THP-1 and HL-60 cell lines were differentiated using phorbol 12-myristate 13-acetate.ERαinhibition was assessed using ELISA.The MTT assay assessed cell viability.Flow cytometry was performed for cell cycle,apoptosis,and p-Akt analyses.Chemical analysis identified the compound as 3-(4-isopropyl)benzylidene-8-ethoxy,6-methyl,chroman-4-one,which showed high binding efficacy toward ER,with aΔG_(binding) score of−7.4 kcal/mol.SBL-060 inhibited ERα,exhibiting IC50 values of 448 and 374.3 nM in THP-1 and HL-60 cells,respectively.Regarding inhibited cell proliferation,GI50 values of SBL-060 were 244.1 and 189.9 nM for THP-1 and HL-60 cells,respectively.In addition,a dose-dependent increase in sub G_(0)/G_(1) phase cell cycle arrest and total apoptosis was observed after treatment with SBL-060 in both cell types.SBL-060 also dose-dependently increased the p-Akt-positive populations in both THP-1 and HL-60 cells.Our results indicate that SBL-060 has excellent efficacy against differentiated AML cell types by inhibiting ER and Akt kinase,warranting further preclinical evaluations.
文摘A new method for the cleavage of carbohydrate benzylidene acetal has been developed using Ceric (YV) ammonium nitrate (CAN) [(NH4)2Ce(NO3)6] in CH3CN-H2O (10/1, v/v).
文摘A versatile and environmentally friendly method for α,α’-bis(substituted ben-zylidene) cycloalkanones has been developed using a heterogeneous catalysis technology. We have synthesized a series of the α,α’-bis(substituted benzylidene) cycloalkanones, a biologically important class of compounds, via the cross aldol condensation between arylaldehydes and cycloketones using sodium-modified fluorapatite (Na/FAP) as a highly efficient solid catalyst under conventional heating in aqueous media and solventless conditions under microwave. Catalyst reuse, ease of separation of the pure product, and high yields are some of the unique features of this process. Shorter reaction times (4 - 7 min) and higher yields (80% - 94%) were achieved under microwave irradiation conditions.
基金the National Natural Science Foundation of China (No. 22071171)the Natural Science Foundation of Zhejiang Province (No. LZ22B020003)
文摘A green and highly efficient strategy for the preparation of bridged spirocyclic compounds via visible-light-induced cyclization of 2-(2-(arylethynyl)benzylidene)malononitrile derivatives with 2,6-di(tert-butyl)-4-methylphenol(BHT)at room temperature was developed.The photoinduced radical reactions generated the corresponding products in good yields under simple and mild reaction conditions.
基金Project supported by the National Natural Science Foundation of China.
文摘An unexpected synthesis of an α, β, γ,δ-unsaturated ketone, which embodies a new type of oxy-carbon cyclic structure, was achieved, while we tried to construct the taxane CB-ring system. Also, a series of abnormal reaction phenomena was found to be related to the formation and reaction of seven membered cyclic benzylidene acetal.
文摘In this work we synthesized new derivatives from Phenyl Hydrazine and series of different Aldehydes (derivatives of benzylidenes). The synthesized compounds contain different aromatic Aldehydes which attached by Benzene ring via Hydrazine moiety in glacial acetic acid. These derivatives were characterized by TLC, melting points, Infrared Red, Proton Nuclear Magnetic Resonance, Carbon Thirteen Nuclear Magnetic Resonance and Mass Spectroscopy. Finally, these synthesized derivatives were tested for antiproliferative activity against multiple normal and cancerous cell lines, HepG2 (Liver cancer) and MCF-7 (Breast cancer) cell lines were used for cytotoxic assay.
文摘In this work, some new oxadiazole derivatives have been prepared, by reacting phenyl hydrazine and acetic anhydride together, which furnished 2,4-dimethyl-4-phenyloxadiazole. This product was reacted with a series of aromatic aldehydes, to obtain a series of oxadiazole derivatives. These derivatives were characterized by TLC, melting points, infrared red, proton nuclear magnetic resonance, carbon thirteen nuclear magnetic resonance and mass spectroscopy. Finally, these synthetized derivatives were tested for antiproliferative activity by two different cell lines. MCF-7 (Breast cancer cell line) and HepG2 (Liver cancer cell line) were used to assess the antiproliferative activity of the prepared compounds.
文摘A versatile synthetic approach toward a series of benzothiazepines with medicinal potential (for example, compound <strong>1</strong>) that allows incorporation of structural variation at the three aromatic regions of the structure, and at the sulfur atom, was developed. Knoevenagel condensation of indan-1,3-diones with benzaldehydes, yielded 2-benzylidineindan-1,3-diones, which undewent thio-Michael addition and intramolecular imine formation upon reaction with 2-aminothiophenols, to produce the target benzothiazepines. Use of indan-1,3-diones, benzaldehydes or 2-aminothiophenols bearing further substitution enabled production of novel 5,11-dihydro-12H-benzo[b]indeno [1,2-e][1,4]thiazepin-12-one analogs <strong>1</strong> - <strong>14</strong>, including compounds bearing substitution at novel positions within the scaffold.
基金Anhui Provincial Teaching Team of Organic Chemistry(2017jxtd051)2019 University Outstanding Young Talents Support Program Project(General Project)of Anhui Province(gxyq2019108)+1 种基金the Major Basic Research Project of the Natural Science Foundation of the Anhui Province Education Department(KJ2016A512)the Natural Science Foundation of Chizhou University(CZ2019ZRZ01)。
文摘A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing ability to 15 metal ions was investigated.Weak emission from TBB could be efficiently increased by trace Hg^2+,through coordination reaction between TBB and Hg^2+ with"turn on"character.The fluorescence intensity of TBB/Hg^2+([TBB]=3.0×10^–6 mol/L,[Hg2+]=1.3×10^–4 mol/L)was 7.5 times higher than that of TBB.This TBB sensor exhibited high selectivity for Hg^2+ and other metal ions did not interfere in this determination.The limit of detection was 0.566μmol/L(S/N=3).The experimental results showed that this TBB sensor could sensitively respond to Hg^2+ within concentration range(from 5×10–6 mol/L to 1.3×10^–4 mol/L).
基金Project supported by the State Science and Technology Committee of China.
文摘Propyl O-(α-L-rhamncpyranosyl)-(1→3)-[2,4-di-O-(2s-methylbutyryl)-α-L-rham-nopyranosyl]-(1→2)-(3-O-acetyl-β-D-glucopyranosyl)-(1→2)-β-D-fucopyranoside (1), the tetrasac-charide moiety of Tricolorin A, was synthesized in total 23 steps with a longest linear sequence of 10 steps, and overall yield of 3.7% from D-Glucose. The isomerization of the dioxolane-type berzyli-dene in the presence of NIS/AgOTf was observed. Tetrasaccharide 1 exhibited no activity against the cultured P388 cell as Tricolorin A did.