Discovery of New Antiproliferative Imidazopyrazole Acylhydrazones Able To Interact with Microtubule Systems

Even though immunotherapy has radically changed the search for anticancer therapies, there are still many different pathways that are open to intervention with traditional small molecules. To expand our investigation in the anticancer field, we report here a new series of compounds in which our previous pyrazole and imidazopyrazole scaffolds are linked to a differently decorated phenyl ring through an acylhydrazone linker. Preliminary tests on the library were performed at the National Cancer Institute (USA) against the full NCI 60 cell panel. The best compounds among the imidazopyrazole series were then tested by immunofluorescence staining for their inhibition of cell proliferation, apoptosis induction, and their effect on the cell cycle and on microtubules. Two compounds, in particular 4-benzyloxy-3-methoxybenzyliden imidazopyrazole-7-carbohydrazide showed good growth inhibition, with IC₅₀ values in the low-micromolar range, and induced apoptosis. Both compounds altered the cell-cycle phases with the appearance of polyploid cells. Immunofluorescence analysis evidenced microtubules alterations; tubulin polymerization assays and docking studies suggested the tubulin system to be the possible, although not exclusive, target of the new acylhydrazone series reported here.     

飞机机械成品试验信息管理系统设计与应用

分析了航空企业飞机机械成品试验的现状,结合企业信息化管理的发展趋势,对飞机机械成品试验的流程进行梳理,基于ASP.NET技术研究开发了某企业飞机机械成品试验数据收集及信息管理系统,以实现飞机机械成品试验的流程化、数字化及显性化管理,避免因试验台管理不善造成的质量问题,实时掌握试验台状态,促进形成自主管理模式。     

基于深度网络迁移学习的致痫区脑电识别* .txt

摘要：致痫区脑电识别能够为癫痫外科手术提供重要的参考价值。提出了一种基于深度网络迁移学习的致痫区脑电识别算法。首先利用连续小波变换（CWT）对脑电信号进行时频分析，获得脑电信号时频图；然后迁移学习AlexNet网络模型，调整网络结构使之适应于致痫区脑电识别，将模型第7层全连接层输出作为脑电信号时频图的特征表示，最后利用支持向量机（SVM）、BP神经网络、长短期记忆网络（LSTM）、基于稀疏表达分类算法（SRC）、线性判别分析（LDA）等分类算法进行特征分类。基于开源脑电数据集采用十折交叉验证的方法对算法进行了验证,比较6种分类器的效果，得到SVM算法的平均特异性为8881%，灵敏度为8807%，准确率为8844%，证明了该方法识别致痫区脑电信号的有效性。 .txt     

一种下肢运动意图识别算法性能实时测评系统* .txt

摘要：对腿部运动意图识别算法的实时性能进行综合可靠的评价是实现下肢假肢灵活稳定控制的前提。提出一种逐层分级的基于下肢运动意图识别算法的实时测评方法，对算法的可靠性、稳定性以及运动意图识别速度进行综合评价。利用开发的运动意图识别算法评测系统，对基于肌电信号源和机械信号源的两种运动意图识别算法进行了实时性能测试，发现肌电信号源的算法识别时间大于机械信号源算法，但是其算法稳定性优于机械信号源算法。进一步地，还利用该评测系统有效地区分出正常识别策略与异常识别策略，发现正常策略的动作识别稳定系数比异常策略高25%左右。因此，所提的基于下肢运动意图识别算法的实时测评方法，能够对不同信号源算法以及不同识别策略的实时性能进行有效评价，为智能下肢假肢控制系统开发提供可供参考的测试平台。 .txt     

厚煤层一次采全高煤壁失稳原因及控制技术

针对成庄煤矿四盘区层一次采全高煤壁失稳问题,对观测统计数据进行分析,发现片帮主要表现形式分五种:顶部、腰部、顶底部、底部以及斜切片帮,据此采用对顶板超前预爆破和煤壁超前预加固技术来控制大采高煤壁稳定性,不仅对煤壁失稳的控制取得了良好的效果,而且经济效益显著。可为相似条件下的厚煤层一次采全高煤壁失稳控制提供借鉴。     

AZ31镁合金薄板经不同累积应变的连续弯曲变形后的显微组织与成形性能

对AZ31镁合金板材进行不同累积应变的连续弯曲变形及退火处理,随后对显微组织与力学性能的变化进行了研究。结果表明:经不同累积应变的连续弯曲变形后,镁合金板材的显微组织中没有发现孪晶,退火后,板材表层的晶粒异常长大,粗晶层的厚度随着累积应变的增加而增加,并且镁合金板材的织构朝RD方向偏转,偏转角度随累积应变的增加而增大;与原始板材相比,连续弯曲变形及退火处理使镁合金板材呈现出较好的室温成形性能(杯突值由2.3 mm提高到4.9 mm,提高了~113%),这主要归因于基面织构的改善使镁合金板材的r值减小与n值增大。     

Calorimetric study of ytterbium orthovanadate YbVO4 polycrystalline ceramics

The heat capacity of ytterbium orthovanadate was first measured by adiabatic calorimetry in the temperature range T?=?12.28–344.06?K. No obvious anomalies were observed on the curve obtained. The values of standard thermodynamic functions in the temperature range T?=?0–400 K were calculated. Based on low-temperature calorimetry data obtained, previously published data on the high-temperature heat capacity of ytterbium orthovanadate were corrected. The anomalous contribution to heat capacity for YbVO₄ was compared with the data known for YbPO₄.     

Synthesis and properties of (Hf1-xTax)C solid solution carbides

Thermodynamically stable (Hf_1–xTa_x)C (x?=?0.1–0.3) compositions were selected by First Principle Calculation and synthesized in nanopowders via high-energy ball milling and carbothermal reduction of commercial oxides at 1450?°C. The formation of a solid solution during powder synthesis was investigated. The solid solution carbide powders were sintered at 1900?°C by spark plasma sintering without a sintering aid. As a result, the (Hf_1–xTa_x)C solid solution carbides exhibited high densities, excellent hardness and fracture toughness (ρ: 98.7–100.0%, HVN: 19.69–19.98?GPa, K_IC: 5.09–5.15?MPa?m^1/2) compared with previously reported HfC and HfC–TaC solid solution carbides.     

Hydrogen production through dry reforming of biogas using a porous electrochemical cell: Effects of a cobalt catalyst in the electrode and mixing of air with biogas

This paper reports the performance of porous Gd-doped ceria (GDC) electrochemical cells with Co metal in both electrodes (cell No. 1) and with Ni metal in the cathode and Co metal in the anode (cell No. 2) for CO₂ decomposition, CH₄ decomposition, and the dry reforming reaction of a biogas with CO₂ gas (CH₄ + CO₂ → 2H₂ + 2CO) or with O₂ gas in air (3CH₄ +?1.875CO₂ +?1.314O₂ → 6H₂ +?4.875CO +?0.7515O₂). GDC cell No. 1 produced H₂ gas at formation rates of 0.055 and 0.33?mL-H₂/(min?m²-electrode) per 1?mL-supplied gas/(min?m²-electrode) at 600?°C and 800?°C, respectively, by the reforming of the biogas with CO₂ gas. Similarly, cell No. 2 produced H₂ gas at formation rates of 0.40?mL-H₂/(min?m²) per 1?mL-supplied gas/(min?m²) at 800?°C from a mixture of biogas and CO₂ gas. The dry reforming of a real biogas with CO₂ or O₂ gas at 800?°C proceeded thermodynamically over the Co or Ni metal catalyst in the cathode of the porous GDC cell. Faraday's law controlled the dry reforming rate of the biogas at 600?°C in cell No. 2. This paper also clarifies the influence of carbon deposition, which originates from CH₄ pyrolysis (CH₄ → C + 2H₂) and disproportionation of CO gas (2CO → C + CO₂), on the cell performance during dry reforming. The dry reforming of a biogas with O₂ molecules from air exhibits high durability because of the oxidation of the deposited carbon by supplied air.