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.     

井下作业面巷道切顶卸压施工设计探究

以井下作业面巷道切顶卸压施工设计为对象开展探究,结合具体工程实际,从切顶卸压爆破施工设计和爆破施工分析两个角度,对切顶卸压技术的全面应用进行总结分析,希望能够为其他矿井相似工程的开展提供借鉴与参考。     

美国全面制裁伊朗对中国能源安全的影响与对策建议

美国自2018年5月宣布重启对伊朗全面制裁,伊朗再次成为国际社会关注的焦点。本文系统梳理了伊朗能源禀赋及开发利用现状,分析了伊朗对中国能源安全的保障程度及其优势,发现1997~2017年伊朗对中国石油安全的保障程度呈波动上升态势,对维护中国油气资源供给安全具有重要意义,认为中伊能源合作具有战略互补性、地缘政治优势、经济优势、历史文化基础和降低美元计价风险等优势。在上述基础上,本文从能源价格、供给渠道和运输安全三方面剖析了此次美国全面制裁伊朗对中国能源安全可能产生的影响,并从规避美国制裁风险和保障国家能源安全角度,提出了相关对策建议。     

渐变刚度板簧式轻卡悬架阻尼参数仿真设计

为了有效提高渐变刚度钢板弹簧式轻型卡车的乘坐舒适性,根据弹簧受力与刚度和变形之间的关系,利用等频原理,建立了渐变刚度钢板弹簧力学特性解析计算模型,并利用钢板弹簧加载-卸载试验对所建立的模型的正确性进行了验证。基于1/2车辆行驶振动模型,利用MATLAB的Simulink工具箱,建立了考虑渐变刚度钢板弹簧力学特性的轻卡行驶振动仿真分析模型。最后,以人体振动舒适性最佳为目标,利用多岛遗传算法,建立了轻卡悬架系统阻尼参数仿真设计方法,并利用实车试验对所建立的轻卡悬架系统阻尼参数仿真设计方法的正确性进行了验证。上述研究为渐变刚度钢板弹簧式轻卡悬架系统参数的设计提供了有效参考。     

基于CDIO工程教育的应用型人才培养 理论与实践研究 — —以红外多路遥控系统设计为例

The construction of specialty groups in higher vocational colleges is in full swing. However, due to the cognitive bias and the lack of construction paradigm for reference, the construction of specialty groups is still in the period of "crossing the river by feeling the stones" with different opinions. There are some problems in the construction of specialty groups, such as unclear under- standing of the concept of specialty groups, unreasonable logic of groups, unclear construction of groups, and nonstandard manage- ment of groups. This paper describes the specific content of the construction of modern information technology specialty group based on the Sydney Agreement, hoping to form a reference paradigm for the construction of specialty group of similar colleges and universities.     

Systematic convergence of nonlinear stochastic estimators on the Special Orthogonal Group SO(3)

This paper introduces two novel nonlinear stochastic attitude estimators developed on the Special Orthogonal Group with the tracking error of the normalized Euclidean distance meeting predefined transient and steady‐state characteristics. The tracking error is confined to initially start within a predetermined large set such that the transient performance is guaranteed to obey dynamically reducing boundaries and decrease smoothly and asymptotically to the origin in probability from almost any initial condition. The proposed estimators produce accurate attitude estimates with remarkable convergence properties using measurements obtained from low‐cost inertial measurement units. The estimators proposed in continuous form are complemented by their discrete versions for the implementation purposes. The simulation results illustrate the effectiveness and robustness of the proposed estimators against uncertain measurements and large initialization error, whether in continuous or discrete form.     

空冷器用高压水清洗与雾化降温系统集成设计与开发

高压水清洗系统和喷淋降温系统分别是春季保持空冷器翅片表面清洁和夏季保证空冷器在高温下正常运行的2个重要辅助系统。针对喷淋系统的缺点研究了高压射流雾化技术,通过试验论证了高压水清洗与雾化降温系统集成的可行性和合理性。根据设计思路开发的集成系统已在山西某项目获得应用并取得了良好的使用效果,此高压水清洗与雾化降温集成系统中高压水发生装置及介质输送管路共用,产生的高压水射流雾化颗粒可达到60μm,夏季降温效果较传统喷淋降温效果大幅提升,水资源的利用率得到极大提高,系统性价比更高。     

基于传统清管球接收器的滤杂防堵工艺设计

清管球回收操作过程中,清管球接收器的泄压、排液和惰化导致泥、砂、垢等杂质积聚在清管球接收器中,并随油气物流进入闭排系统管线,造成杂质流失、闭排系统管线堵塞和压力无法完全释放,影响对海底油气管道腐蚀、析蜡、结垢及地层出砂等情况的判断,存在很大的安全隐患。通过对清管球接收器实施工艺改造,使清管球接收器具备滤杂防堵功能和自动取样功能,有效解决了闭排管线堵塞、杂质流失和安全隐患问题。该工艺研究对于海上油气田海底管线的运营和维护具有较高的借鉴意义。     

解析“限额设计”措施对建设项目投资的控制对策

经济新常态下,我国建筑行业得到快速发展。对于建筑工程来说,为节约成本,在"限额设计"思想指导下,必须开展精细化管理,从而提高项目投资的控制能力。然而,在项目建设过程中对于"限额设计"措施的利用水平并不高,不利于企业的可持续发展。因此,本文在分析"限额设计"措施的基础上,提出对建设项目投资的控制对策,希望能够对相关施工管理人员提供借鉴。     

Design and characteristics of a new type laminar plasma torch for materials processing

Laminar plasma jet(LPJ) generated by laminar plasma torch(LPT) has a favorable temperature and velocity distribution. Thus, it is superior to the turbulent plasma jet in material processing.However, most of the reported LPTs usually operate at a relatively low output power with a relatively low arc voltage and thermal efficiency, which limits its capabilities. In this context, this paper attempts to design a new type of high-power LPT with a relatively low arc current and a high thermal efficiency. In the first section, the design principle of the main components is studied and discussed in detail, and a new high-power LPT is proposed. Then, the experimental characteristics of the proposed high-power LPT are examined. Experimental results reveal the following characteristics of the proposed LPT.(1) The max jet length of the proposed LPT reaches at 540 mm.(2) Its mean arc voltage is higher than 290 V when the LPT works with arc currents lower than 200 A, leading to an output power greater than 50 kW.(3) The mean thermal efficiency is higher than 50%. Lastly, the proposed LPT has been applied to spheroidize the aluminum oxide powers. The experiment results for the production of spherical powders show that the proposed LPT has a good characteristic for material processing.