CANADIAN JOURNAL OF CHEMICAL ENGINEERING
·
2025
·
IF 1.9
Yu-cheng Jiang,Bao-guang Zhu,Xiang-li Long
The oxidation of 1-(4-chlorophenyl)-pyrazolidin-3-one to 1-(4-chlorophenyl)-1H- pyrazol-3-ol by air can be accelerated by the Co(II)@AC catalyst prepared by loading Co(II) on activated carbon with wet impregnation method. ZnCl 2 solution has been used to treat activated carbon to ameliorate the catalytic ability of Co(II)@AC catalyst. The experiments indicate that the optimal catalyst is made by immersing activated carbon in 0.7 mol/L ZnCl 2 solution at 50°C for 6 h with a liquid/solid ratio of 30/1 (mL/g) followed being calcined at 700°C for 5 h at a heating rate of 5°C/min under N 2 protection. The 1-(4-chlorophenyl)-1H-pyrazol-3-ol concentration catalyzed by the catalyst loaded on the best carbon reaches 0.01953 kg/L, which is 27.56% higher than that catalyzed by the catalyst loaded on the original carbon. The characterization results manifest that the modification with ZnCl 2 enriches the porous structure and increases the acidic groups on the surface of activated carbon. The conversion of 1-(4-chlorophenyl)-pyrazolidin-3-one is mainly determined by the physical structure of the activated carbon while the selectivity to 1-(4-chlorophenyl)-1H- pyrazol-3-ol is largely affected by the chemical characteristics of the activated carbon.
研究领域:
化学
·
催化材料科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2023
·
IF 3.8
Junjie Wang,Hui Zhou,Yang Li,Yeshu Mu,Jinghua Li,Chen Hong,Wen Luo
A novel series of benzo[ cd ]indol-2(1 H )-one-donepezil (BIO-DPZ) hybrids (5a-m, 6a-k) was designed, synthesized and evaluated as cholinesterase inhibitors and living cell imaging agents. These compounds were potent inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Compound 6a exhibited the strongest inhibitory activity against AChE with an IC 50 value of 0.16 μM. Compound 6i had the strongest inhibition of BuChE with an IC 50 value of 5.37 μM. Kinetic and molecular modeling studies showed that 6a bound both catalytic active site and peripheral anionic site of AChE. Compounds 6a and 6i both showed lower SH-SY5Y, HepG2 and HL-7702 cytotoxicity than the mitoxantrone. Promisingly, the most active compound, 6a, was successfully used in living SH-SY5Y cell imaging and had predictable lipophilicity and blood-brain-barrier permeation properties. These hybrids should undergo further systematic study in the treatment of Alzheimer's disease.
研究领域:
药理学
·
神经科学
·
药物化学
✓ 已验证
DOI
高影响因子
BIOORGANIC CHEMISTRY
·
2023
·
IF 5.1
Shuai Wang,Jian-Tao Shi,Xing-Rong Wang,Hong-Xia Mu,Xue-Ting Wang,Kai-Yan Xu,Qing-Shan Wang,Shi-Wu Chen
The PI3K/AKT/mTOR signaling pathway is one of the most common abnormal activation pathways in tumor cells, and has associated with multiple functions such as tumor cell growth, proliferation, migration, invasion, and tumor angiogenesis. Here, a series of 3-amino-1 H -indazole derivatives were synthesized, and their antiproliferative activities against HT-29, MCF-7, A-549, HepG2 and HGC-27 cells were evaluated. Among them, W24 exhibited the broad-spectrum antiproliferative activity against four cancer cells with IC 50 values of 0.43–3.88 μM. Mechanism studies revealed that W24 inhibited proliferation by affecting the DNA synthesis, induced G 2 /M cell cycle arrest and apoptosis by regulating Cyclin B1, BAD and Bcl-xL, meanwhile induced the change of intracellular ROS and mitochondrial membrane potential in HGC-27 cells. Moreover, W24 inhibited the migration and invasion of HGC-27 cells by decreasing EMT pathway related proteins and reducing the mRNA expression levels of Snail, Slug and HIF-1α. Furthermore, W24 displayed low tissue toxicity profile and good pharmacokinetic properties in vivo . Therefore, 3-amino-1 H -indazole derivatives might serve as a new scaffold for the development of PI3K/AKT/mTOR inhibitor and anti-gastric cancer reagent.
研究领域:
肿瘤学
·
药理学
·
化学
·
细胞生物学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHYSICA STATUS SOLIDI A-APPLICATIONS AND MATERIALS SCIENCE
·
2021
·Vol. 219
·期 3
·2100568
·
IF 1.981
Ling Lan,Haidou Wang,Lina Zhu,Yuelan Di,Jiajie Kang,Junhong Qiu
Herein, a grid-like microstructure is prepared on the surface of 3Cr13 stainless steel through nanosecond laser etching, and the self-assembled 1 H ,1 H ,2 H ,2 H -perfluorodecyltriethoxysilane (PFDS) coating is further composited to prepare a superhydrophobic surface with a contact angle of 164° and a rolling angle of 3°. The effect of laser etching cycles on the surface microstructure and surface wettability before and after the self-assembly is studied. With an increase in the etching cycles, a stable grid-like microstructure is gradually formed on the surface, and subsequently, a composite structure of grooves and pits is formed. After the self-assembly of the PFDS coating, two superhydrophobic surfaces with different wetting properties are obtained. Furthermore, as the etching cycles increase, the surface changes from a superhydrophobic and high-adhesion state to a superhydrophobic and low-adhesion state. The decrease in surface energy is mainly attributed to the C−F group in the PFDS molecule. The experimental results show that PFDS molecules are deposited easily in case of the convex surface, thereby facilitating the formation of superhydrophobic low-adhesion surfaces. Finally, the superhydrophobic surface is still maintained after cumulative ultrasonic cleaning in deionized water for 75 min, showing good reusability and stability.
研究领域:
材料科学
·
表面工程学
✓ 已验证
DOI
高影响因子
POLYMER COMPOSITES
·
2025
·
IF 4.7
Tengyang Zhang,Jie Fei,Jifeng Yan,Zhaoxi Gou,Peng Cheng,Lehua Qi
At low temperature (−60°C), increased brittleness and surface grease adhesion promote significant adhesive wear in the composites. 1H,1H,2H,2H-perfluorooctane trichlorosilane (PFOTS) was coated onto carbon fibers to enhance the tribological performance at low temperature of the composites. Compared to the original material, the shear strength of the modified sample was increased by 31.9% to 20.16 MPa, while the wear rate under −60°C was decreased significantly by 87.5% to 1.72 × 10 −8 cm 3 /J. The low-temperature adhesive wear mechanisms were first revealed by combining experimental measurements with molecular dynamics simulations, and the simulations further clarified how a PFOTS coating modifies the tribological response of the material.
研究领域:
材料科学
·
复合材料工程
·
表面科学
·
摩擦学
·
低温工程
✓ 已验证
产品关联
DOI
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2025
·
IF 5.4
Yeming Huang,Jingxuan Zhang,Renhong Wang,Bing Gao,Ruyi Miao,Sirun Zhang,Dunju Wang
Improving the energy release efficiency of aluminium powders in weaponry is essential. In this study, uniform core-shell Al@(PFDTES/GAP) was prepared by hydrolyzing PFDTES and co-reacting it with GAP on aluminum powder. It showed better thermal reaction, combustion and energy release. The thermal properties of Al@(PFDTES/GAP) exhibit a significant aluminum-fluorine exothermic phenomenon in DSC, with a 4.9 % increase in exothermic heat in the combustion test compared to raw-Al. For the samples blended with PTFE, Al@(PFDTES/GAP)/PTFE demonstrated excellent performance in terms of increased heat release (increased by 28.0 %) in DSC, higher heat release (increased by 10.2 %) in the heat of combustion test, larger combustion flame area and faster combustion speed (the time reduced by 20.0 %) in the air, compared with that of raw-Al/PTFE. In conclusion, this method is simple and effective to enhance the energy release of aluminium powder, which is of great significance for improving the energy of weapons and equipment.
研究领域:
材料科学
·
能源工程
✓ 已验证
产品关联
DOI
高影响因子
Frontiers in Pharmacology
·
2021
·
IF 5.811
Xiao Qing,Liu Qi-Meng,Jiang Ru-Chao,Chen Kai-Feng,Zhu Xiang,Ma Lei,Li Wei-Xi,He Fei,Huang Jun-Jun
Previous studies have indicated that α1D/1A antagonist naftopidil (NAF) suppresses prostate growth by decreasing cell proliferation without affecting apoptosis and prostate volume in benign prostatic hyperplasia (BPH). A NAF-derived α1D/1A antagonist 1- benzyl-N-(3-(4-(2-methoxyphenyl) piperazine-1-yl) propyl)-1H-indole-2- carboxamide (HJZ-12) has been reported from our laboratory, which exhibits high subtype-selectivity to both α1D- and α1A- AR (47.9- and 19.1- fold, respectively) with respect to a1B-AR in vitro. However, no further study was conducted. In the present study, a pharmacological evaluation of HJZ-12 in BPH was performed on an estrogen/androgen-induced rat BPH model and human BPH-1 cell line. In vivo, HJZ-12 exhibited better performance than NAF in preventing the progression of rat prostatic hyperplasia by not only decreasing prostate weight and proliferation (similar to NAF) but also, shrinking prostate volume and inducing prostate apoptosis (different from NAF). In vitro, HJZ-12 exhibited significant cell viability inhibition and apoptotic induction in BPH-1 cell line, without presenting cell anti-proliferation properties. Intriguingly, the role of HJZ-12 on cell viability and apoptosis was an α1-independent action. Furthermore, RNA-Seq analysis was applied to screen out six anti-apoptotic genes (Bcl-3, B-lymphoma Mo-MLV insertion region 1 [Bmi-1], ITGA2, FGFR3, RRS1, and SGK1). Amongst them, Bmi-1 was involved in the apoptotic induction of HJZ-12 in BPH-1. Overall, HJZ-12 played a remarkable role in preventing the progression of prostatic hyperplasia through α1-independent apoptotic induction, indicating that it will be a multi-target effective candidate for BPH treatment.
研究领域:
药理学
·
泌尿学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
·
2014
·
IF 2.129
Zhijian Che,Shaoxiang Wang,Shenggui Liu,Guobi Li,Qiting Wu,Chunyu Lin,Linglang Kong,Sheng Wang
A new complex [Zn(bbb)Cl 2 ]·DMF, where bbb is 2-(2-(1H-benzo[ d ]imidazol-2-yl)benzyl)-1H-benzo[ d ]imidazole, was synthesized and characterized by element analysis, 1 H NMR and X-ray single crystal structure analyses. For complex: crystal system, triclinic, space group, P – 1 , a = 9.4661(13), b = 10.3534(14), c = 13.0025(18) Å, α = 73.477(2), β = 80.743(2), γ = 88.658(2)°, V = 1205.5(3) Å 3 , Z = 2. In this complex, the Zn 2+ distorted tetrahedron geometry is coordinated by two nitrogen atoms from 2-(2-(1H-benzo[ d ]imidazol-2-yl)benzyl)-1H-benzo[ d ]imidazole and two Cl − . The complex emits yellow green luminescence with the maximal emission peak at 550 nm in DMF solution. The complex exhibits inhibition on the growth of Eca109 cancer cell with IC 50 value of 8.9 ± 1.1 μM, which was lower than that of cisplatin (14.3 ± 1.4 μM). This complex has potential application in treatment of esophageal cancer.
研究领域:
无机化学
·
药物化学
·
材料科学
·
生物无机化学
·
药物研究
✓ 已验证
DOI
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2021
·
IF 6.514
Xing-Rong Wang,Shuai Wang,Wen-Bo Li,Kai-Yan Xu,Xue-Peng Qiao,Xue-Li Jing,Zi-Xiao Wang,Chang-jiang Yang,Shi-Wu Chen
Vascular endothelial growth factor-2 (VEGFR-2) plays a pivotal role in tumor angiogenesis . Herein, a library of novel 2-(4-(1 H -indazol-6-yl)-1 H -pyrazol -1-yl)acetamide derivatives were designed and synthesized as VEGFR-2 inhibitors based on scaffold hopping strategy. These compounds exhibited the excellent inhibitory in both VEGFR-2 and tumor cells proliferation . Especially, compound W13 possessed potent VEGFR-2 inhibition with IC 50 = 1.6 nM and anti-proliferation against HGC-27 tumor cells with IC 50 = 0.36 ± 0.11 μM, as well as less toxicity against normal GES-1 cells with IC 50 = 187.46 ± 10.13 μM. Moreover, W13 obviously inhibited colony formation, migration and invasion of HGC-27 cells by adjusting the expression of MMP-9 and E-cadherin, and induced HGC-27 cells apoptosis by increasing ROS production and regulating the expression of apoptotic proteins. Furthermore, W13 blocked the PI3K-Akt-mTOR signaling pathway in HGC-27 cells. In addition, anti-angiogenesis of W13 was proved by inhibiting tube formation and the expression of p-VEGFR-2 in HUVEC cells. All the results demonstrated that W13 could be developing as a promising anticancer agent for gastric cancer therapy.
✓ 已验证
DOI
PubMed
高影响因子
Journal of Food Measurement and Characterization
·
2021
·Vol. 15
·期 3
·2716-2726
·
IF 2.431
Qian Junqing,Zhao Changyan,Zhu Hanxiao,Tong Jun,Zhao Xiaohua,Yang Haiyan,Guo Hui
Walnut oil is endowed with a variety of physiological functions due to abundant natural compounds, and the effect of unsaturated fatty acids is crucial. In order to accurately and conveniently detect the fatty acids components and content in walnut oil, a quantitative method was developed to detect fatty acids content based on the 1 H-NMR and 13 C-NMR techniques. In addition, HPLC combined with MS was used to conduct qualitative analysis. HPLC method with an evaporative light-scattering detector was for the quantitative analysis and the fatty acids content was compared with the content from NMR. The result showed that there was no significant difference between 1 H-NMR, 13 C-NMR and HPLC (P > 0.05) and indicated that the NMR has the potential to be applied as a routine method for the analysis of fatty acids content in walnut oil.
研究领域:
分析化学
·
食品科学
·
营养学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Ocean University of China
·
2025
·Vol. 24
·期 6
·1827-1833
·
IF 1.2
Xin Wenyuan,Zhou Yunbing,Liu Daixi,Wang Cong,Sherwin K. B. Sy
Astaxanthin (AX) and vitamin E (VE) are widely consumed nutritional supplements in China, with its beneficial effects predominantly attributed to all-trans AX and VE. The aim of this study is to develop and validate a rapid and accurate method for quantifying the content of AX and VE in nutritional supplement products using highly sensitive 1 H NMR method. Coumarin was chosen as the internal standard. Specific signals from AX was optimal at H-7,7′ in the chemical shift range of δ 6.17–6.24 ppm, whereas the signals of VE at δ 2.59 ppm. To demonstrate the reliability of this analytical approach the proposed method underwent rigorous validation, specificity, limit of detection (LOD), limit of quantitation (LOQ), linearity, accuracy, precision, and recovery. The accuracy of the validation method was 3.10% for AX and 1.99% for VE. The results indicated that the method was precise and reliable. The method has been successfully applied to simultaneous quantification of AX and VE in nutritional supplements products.
研究领域:
分析化学
·
营养科学
·
药物分析
✓ 已验证
产品关联
DOI
高影响因子
Separations
·
2022
·Vol. 9
·期 12
·388
·
IF 3.344
Yulin You,Dongxiao Guo,Weiliang Cui,Zhifan Wang,Chunguo Yang,Yongqiang Lin,Shuqi Wang
Matrix-assisted diffusion-ordered spectroscopy (MA DOSY) technology enables efficient the virtual separation of components in a mixture according to their coefficients (D). In the current research, MA DOSY technology was applied for the analysis of a flavonoid mixture. To establish the method, five representative active flavonoid ingredients, including baicalein, baicalin, quercetin, puerarin and rutinum, were selected for the mixture model. The effects of the type and concentration of the matrix, solvent polarity, and nuclear magnetic resonance (NMR) experimental conditions on the resolution of the DOSY spectrum were investigated. It turned out that sodium dodecyl sulfate (SDS) showed the best performance in increasing the resolution of different analytes, which initially increased to the peak below the added amount of 9 mg, and decreased upon the addition of more SDS. In addition, the five flavonoids showed higher resolution in DMSO–d6than in MeOD. Experimental parameters of DOSY, including the number of scans (NS), dummy scans (DS), and value of the FID data points (TD), were also optimized. Finally, the above optimized method was used for the qualitative analysis of the total flavonoid mixture extracted fromScutellaria baicalensisGeorgi. A total of nine compounds were identified and confirmed by comparing them with mass spectrometry data, which further verifies the practical value of this method upon analyzing flavonoid mixtures and provides some reference significance for the follow-up research.Keywords:NMR;MA-DOSY;flavonoids;mixture separation
研究领域:
分析化学
·
药学
·
天然产物化学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）