ORGANIC & BIOMOLECULAR CHEMISTRY
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2022
·Vol. 20
·期 25
·5104-5114
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IF 3.89
Jin-Rong Lai,Fu-Dan Yin,Qing-Song Guo,Fei Yuan,Bei-Fang Nian,Ming Zhang,Zhi-Bang Wu,Hong-Bin Zhang,E Tang
An Ag-catalysed three-component reaction of alkynyl aryl ketones bearing an ortho-methoxy group, element selenium, and arylboronic acid, providing a facile route to selenofunctionalized chromone products has been developed. This protocol features high efficiency and high regioselectivity, and the use of selenium powder as the selenium source. Mechanistic experiments indicated that the combined oxidative effect of (bis(trifluoroacetoxy)iodo)benzene and oxygen in the air pushes the catalytic redox cycle of the Ag catalyst and the phenylselenium trifluoroacetate formed in situ is the key intermediate of the PIFA-mediated 6-endo-electrophilic cyclization and selenofunctionalization reaction of alkynyl aryl ketones.
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2019
·
IF 2.931
Yujia Xu,Taotao Dai,Ti Li,Kechou Huang,Yuting Li,Chengmei Liu,Jun Chen
The interaction between plant protein and polyphenol is a topic of considerable interest. However, there is relatively little understanding about the interaction between rice protein and epigallocatechin-3-gallate (EGCG). The spectroscopy and computational docking program were used to investigate the potential interaction between rice glutelin (RG) and EGCG. It was found that the intrinsic fluorescence of RG could be quenched by EGCG, which indicated interaction occurred between them. Thermodynamic analysis elucidated that the interaction process between RG and EGCG happened spontaneously with hydrogen bond as the primary driving force. The ANS-fluorescence indicated that the surface hydrophobicity of RG reduced with the increasing of EGCG. Circular dichroism spectra and synchronous fluorescence gave further information for the conformational and microenvironmental changes of RG. Particularly, the α-helix structure reduced and random coil structure increased after the binding interaction. Furthermore, the computational docking program exhibited target sites in which the amino acid residues of RG and EGCG might be bound together.
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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2021
·
IF 5.051
Xiang Zhou,Jiamin Liu,Jiao Meng,Yihong Fu,Zhibin Wu,Guiping Ouyang,Zhenchao Wang
Microtubule dynamics are crucial for multiple cell functions, and cancer cells are particularly sensitive to microtubule-modulating agents. Here, we describe the design and synthesis of a series of (Z)-2-(5-benzylidene-4-oxo-2-thioxothiazolidin-3-yl)-N-phenylacetamide derivatives and evaluation of their microtubule-modulating and anticancer activities in vitro. Proliferation assays identified I20 as the most potent of the antiproliferative compounds, with 50% inhibitory concentrations ranging from 7.0 to 20.3 µM with A549, PC-3, and HepG2 human cancer cell lines. Compound I20 also disrupted cancer A549 cell migration in a concentration-dependent manner. Immunofluorescence microscopy, transmission electron microscopy, and tubulin polymerisation assays suggested that compound I20 promoted protofilament assembly. In support of this possibility, computational docking studies revealed a strong interaction between compound I20 and tubulin Arg β369, which is also the binding site for the anticancer drug Taxol. Our results suggest that (Z)-2-(5-benzylidene-4-oxo-2-thioxothiazolidin-3-yl)-N-phenylacetamide derivatives could have utility for the development of microtubule-stabilising therapeutic agents.
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Materials Science and Engineering B-Advanced Functional Solid-State Materials
·
2021
·
IF 4.051
Zhihao Chen,Haiyang He,Zhuoqi Wen,Zhongjie Cui,Shiliang Mei,Dan Yang,Xian Wei,Wanlu Zhang,Fengxian Xie,Bobo Yang,Ruiqian Guo
Broadband emission Mn 2+ doped lead halide perovskites are deemed as promising phosphor materials for solid state white light-emitting-diodes (WLEDs). Herein, we report a facile gram-scale synthesis of Mn-doped CsPb(Br/Cl) 3 phosphors by doping MnCl 2 into CsPbBr 3 perovskite nanocrystals at room temperature. The obtained phosphors present dual-color emission with blue emission at 463 nm and red emission at 602 nm. Increasing MnCl 2 doping amount can enhance the red emission while more 3-Aminopropyltrimethoxysilane (APTMS) ligands can repress Mn related impurity and provide high stability. Further, two kinds of WLEDs (monocomponnet and two-component) are demonstrated. The monocomponent WLED exhibits warm white light under various driving currents (30 mA–150 mA), and the two-component WLED shows good chromatic performance close to ideal white light (0.33, 0.33), demonstrating their potential applications in WLED devices.
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ARCHIV DER PHARMAZIE
·
2019
·Vol. 353
·期 2
·1900231
·
IF 2.145
Xiujie Liu,Xin Chen,Kai Qiu,Zhihao Zhang
A series of 4-methoxy-3-arylamido- N -(substitutedphenyl)benzamides 6a – u were designed according to the splicing principle of structural design in the medicinal chemistry theory and were synthesized in five steps: nitration, acylation, ammoniation, reduction, and secondary ammoniation. The structures of the target compounds were characterized and verified by infrared, 1 H nuclear magnetic resonance (NMR), 13 C NMR, and electron spray ionization spectroscopy. Their in vitro antiplatelet aggregation activities induced by adenosine diphosphate (ADP) or arachidonic acid (AA) were assessed by Born's method. The biological evaluation revealed that all compounds exhibited certain levels of activities in both of the antiplatelet aggregation assays; compounds 6c (IC 50 = 3.84 μM) and 6f (IC 50 = 3.12 μM) displayed the strongest antiplatelet aggregation activities in the ADP-induced and AA-induced assay, separately. Moreover, compounds that had stronger activities were chosen for cell toxicity testing via the cell counting kit-8 assay. The results indicated that none of the compounds had obvious cell toxicity against L929 cells at the doses of 10 and 20 μM. It is worth pointing out that compound 6c showed the highest antiplatelet activity and the lowest cell toxicity. In general, 4-methoxy-3-arylamido- N -(substitutedphenyl)benzamides have the potential to become a kind of safer and more effective antiplatelet agents.
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ACS Applied Optical Materials
·
2025
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IF 3.8
Lipeng Huang,Yanjie Liang,Xulong Lv,Xihui Shan,Yi Zhang,Xiao-Jun Wang
Short-wave infrared (SWIR) light sources, as crucial components of SWIR imaging and spectroscopy technologies, have garnered significant attention recently. The rapid development of portable electronic devices has created a demand for compact and efficient SWIR emitters, and phosphor-converted SWIR LEDs represent the optimal technological solution to meet this requirement. Here, a Cr(PO3)3:Yb3+ phosphor with highly efficient and pure SWIR luminescence under 450 nm blue LED excitation is reported. Upon doping with Yb3+ in the Cr(PO3)3 matrix, the resulting material is capable of effectively converting blue excitation photons to SWIR luminescence spanning from 900 to 1200 nm, with a dominant emission peak at 1003 nm due to the efficient energy transfer from Cr3+ to Yb3+. Notably, this phosphor demonstrates an ultrahigh internal quantum efficiency (IQE) of 95.7% and a record external quantum efficiency (EQE) of 60.3% upon 450 nm blue light excitation. Moreover, the fabricated SWIR LED prototype device by combining the Cr(PO3)3:Yb3+ phosphor and a commercial 450 nm blue LED chip exhibits SWIR output power of 24.1 mW at 200 mA input current and a photoelectric conversion efficiency of 12.8% at 20 mA. This study not only opens avenues for realizing high-efficiency SWIR luminescence by deliberately controlling energy transfer pathways in Cr-based material systems but also paves the way for the development of high-power SWIR light sources.
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JOURNAL OF MATERIALS SCIENCE-MATERIALS IN ELECTRONICS
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2025
·Vol. 36
·期 34
·2170
·
IF 2.8
Wang Yan,Su Congxue,Tao Wenlong,Chen Zelong,Fan Jun,Cheng Min,Chen Beiyi,Zhou Huanfu,Sun Yuan
In light of advancements in 5G/6G technologies, current research on microwave dielectric ceramics is focused on the development of materials characterized by low sintering temperatures and low permittivity, in order to satisfy the requirements of high-frequency low-temperature co-fired ceramic (LTCC) applications. Novel monoclinic structure GdBaK(MoO 4 ) 3 and YBaK(MoO 4 ) 3 ceramics, with C2 / c space group, were synthesized using a conventional solid-state method. GdBaK(MoO 4 ) 3 and YBaK(MoO 4 ) 3 ceramics were sintered at 830 °C and 850 °C, exhibited ε r ~ 8.54 and 8.77, τ f ~ − 51.1 ppm/°C and − 45.8 ppm/°C, Q × f ~ 23, 240 GHz and 59, 277 GHz, respectively. The compression from Ba 2+ and K + cations was identified as the main reason for the higher theoretical ε theo compared to the corrected ε corr . The dielectric loss of both ceramics is mainly affected by the density and packing fraction. The full width at half maximum (FWHM) values of the vibrational peak at 932 cm −1 , corresponding to the symmetric stretching modes of MoO 4 2− , exhibits a negative correlation with the Q × f values. Based on the P–V–L theory, the lattice energy and bond energy associated with the Mo–O bond played a substantial role in influencing the Q × f and τ f . Moreover, YBaK(MoO 4 ) 3 showed good chemical compatibility with Ag, indicating its potential for LTCC applications.
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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2025
·
IF 5.4
Wen Xu,Yujing Zhang,Qianqian Xu,Haibo Zhao,Qun Gao,Xinyu Zhao,Hongfei Jiang,Chao Wang
Microtubules, composed of tubulin subunits, represent a critical target in anticancer drug discovery. The design and evaluation of small-molecule inhibitors targeting tubulin polymerisation continue to hold significant promise for advancing cancer therapeutics. Based on structural insights into tubulin polymerisation inhibitors and tubulin interaction models, a novel series of 3-aryl-4-(3,4,5-trimethoxyphenyl)selenophene derivatives were designed as potential tubulin polymerisation inhibitors. Among the synthesised analogs, compound 7i, featuring a selenophene linker, demonstrated superior antiproliferative activity against Huh7, MCF-7, and SGC-7901 cancer cell lines, with IC50 values slightly lower than those of combretastatin A-4 (CA-4). Structure-activity relationship studies revealed that electron-donating substituents at the para-position of the B-ring significantly enhanced cytotoxic potency. Mechanistic studies revealed that compound 7i effectively inhibited tubulin polymerisation, disrupted microtubule networks, induced G2/M cell cycle arrest, and triggered apoptosis in cancer cells. These results underscore the potential of incorporating selenophene into the CA-4 scaffold as a promising strategy for developing potent tubulin polymerisation inhibitors, offering new avenues for cancer therapy.
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BIOMEDICINE & PHARMACOTHERAPY
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2024
·
IF 6.9
Junyu Wang,Chaojie Yang,Zhixin Liang,Junping Sun,Mingyue Zhang,Shaofu Qiu,Xinying Du,Xi He,Xiaoying Pang,Xidong Ma,Mei Xie,Xinjie Han,Ru Fan,Enlu Zhou,Hairong Yu,Danyang She,Hongbin Song,Jianxin Wang
Human adenovirus (HAdV) infection is a major cause of respiratory disease, yet no antiviral drugs have been approved for its treatment. Herein, we evaluated the antiviral and anti-inflammatory effects of cyclin-dependent protein kinase (CDK) inhibitor indirubin-3′-monoxime (IM) against HAdV infection in cells and a transgenic mouse model. After evaluating its cytotoxicity, cytopathic effect reduction, antiviral replication kinetics, and viral yield reduction assays were performed to assess the anti-HAdV activity of IM. Quantitative real-time polymerase chain reaction (qPCR), quantitative reverse transcription PCR (qRT-PCR), and western blotting were used to assess the effects of IM on HAdV DNA replication, transcription, and protein expression, respectively. IM significantly inhibited HAdV DNA replication as well as E1A and Hexon transcription, in addition to significantly suppressing the phosphorylation of the RNA polymerase II C-terminal domain (CTD). IM mitigated body weight loss, reduced viral burden, and lung injury, decreasing cytokine and chemokine secretion to a greater extent than cidofovir. Altogether, IM inhibits HAdV replication by downregulating CTD phosphorylation to suppress viral infection and corresponding innate immune reactions as a promising therapeutic agent.
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DESIGNED MONOMERS AND POLYMERS
·
2017
·
IF 1.139
Yazhen Wang,Yutao Di,Shaobo Dong,Zijian He,Xueze Zhang,Jia Shi,Tianyu Lan
(3-(tert-butylperoxy)propyl) trimethoxysilane (TBPT), is a tailor-made new style silane coupling agent with peroxide group, which have ability of initiating polymerization. This study used TBPT to generate free radical, and initiated the polymerization of acrylonitrile (AN), thereby forming polyacrylonitrile (PAN) in two approaches, thermal initiation system and redox initiation system. Meanwhile this study bonded TBPT onto nano-TiO2 to get modified nano-TiO2 by means of the coupling function of TBPT, and then made the peroxide group of the modified nano-TiO2 decompose and initiate the polymerization of AN in thermal initiation system and redox initiation system respectively. The products were investigated and analyzed by FTIR, XPS and TG. The result showed that on one hand, in the products of the thermal initiation there was PAN, which both attached and unattached to the modified nano-TiO2; on the other hand, in the products of the redox initiation system the PAN unattached to the modified nano-TiO2 was produced, while the PAN attached to the modified nano-TiO2 was not.
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JOURNAL OF MOLECULAR LIQUIDS
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2020
·
IF 5.065
Hong Li,Yuhao Zhang,Dexin Sun,Liang Zhao,Jinsen Gao,Chunming Xu
In order to investigate the ability of N -methyl-2-pyrrolidone (NMP) to extract aromatics (benzene, toluene) and sulfides (3-methylthiophene, thiophene) from n-hexane, the liquid-liquid equilibrium (LLE) data of n-hexane + {benzene, toluene, thiophene or 3-methylthiophene} + NMP systems were determined at 293.15 K under 101.3 kPa. The Othmer-Tobias and Hand equations were applied to validate the reliability of the obtained LLE data, and the correlation coefficients ( R 2 ) are close to unity. It was found that sulfides could be successfully extracted from n-hexane by NMP solvent companying with the extraction of aromatics. However, the separation factors and distribution coefficients of the sulfides are greater than those of aromatics, indicating that the sulfides are more easily extracted by NMP. Furthermore, the separation energies of the sulfides are greater than that of aromatics, which is also a piece of evidence for easier separation of sulfides. In order to extend those results to other extraction processes involving those sulfides, aromatics and solvent, the binary interaction parameters of the NRTL and UNIQUAC thermodynamic models were calculated by correlating the LLE data. The RMSD values were all <0.0070, and a graphical user interface based on the Gibbs tangent plane test was also applied to validate the coherent consistency of the parameters. The results show that the obtained binary interaction parameters could be reliable adopted in the design and optimization of the related extraction/separation process in industry.
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JOURNAL OF HAZARDOUS MATERIALS
·
2010
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IF 4.144
Lejin Xu,Jianlong Wang
The removal of biocide 4-chloro-3-methyl phenol (CMP) was investigated by heterogeneous Fenton-like system using nanoparticulate zero-valent iron (nZVI) as catalyst. The properties of nZVI before and after reaction were characterized by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The effects of pH value, initial concentration of CMP, nZVI dose and hydrogen peroxide (H 2 O 2 ) concentration were determined. The experimental results showed that lower pH value and CMP concentration brought faster degradation rate. With the initial pH value of 6.1 and initial CMP concentration of 0.7 mM, the optimal dosage of reagents were 0.5 g nZVI/L and 3.0 mM H 2 O 2 . At pH 6.1, the degradation of CMP followed two-stage first-order kinetic that composed of an induction period (first-stage) and a followed rapid degradation stage (second-stage). According to the effects of scavengers n -butanol and KI, hydroxyl radicals ( OH), especially the surface-bounded •OH, had a dominant role in the oxidation of CMP. The degradation intermediates, carboxylic acids and chloride ion produced during the reaction process were monitored by high performance liquid chromatography (HPLC), liquid chromatography/mass spectrometry (LC/MS) and ion chromatography (IC). On the basis of these findings, the possible mechanistic steps of CMP degradation were proposed.
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