Het(aryl)isatin to het(aryl)aminoindoline scaffold hopping: A route to selective inhibitors of matrix metalloproteinases

Matrix metalloproteinases (MMPs) are a large family of zinc-dependent endoproteases known to exert multiple regulatory roles in tumor progression. A variety of chemical classes have been explored for targeting individual MMP isoforms. In the present study, we further developed our isatin based scaffold BB0223107 capable of binding to and inactivating MMP-2 in a zinc-independent manner (Agamennone et al., 2016). Forty four new compounds were synthesized based on the modified BB0223107. All compounds were tested in enzyme inhibition assays against MMP-2, ?8 and ?13. SAR studies demonstrated that 5-het(aryl)-3-aminoindolin-2-ones (37–39) were active toward MMP-2 and MMP-13. The most potent compounds 33 and 37 displayed an IC₅₀ of 3 µM against MMP-13 and showed a negligible activity toward MMP-8; almost all new compounds were inactive toward MMP-8. Replacement of the isatin ring with a biaryl system (compound 33) did not decrease the potency against MMP-13 but reduced the selectivity. Structure-based computational studies were carried out to rationalize the inhibitory activity data. The analysis of binding geometries confirmed that all fragments occupied the S1′ site in the three enzymes while no ligand was able to bind the catalytic zinc ion. To the best of our knowledge, this is the first example of 3-aminoindolin-2-one-based MMP inhibitors that, based on the computer modeling study, do not coordinate the zinc ion. Thus, the het(aryl)-3-aminoindolin-2-one derivatives emerge as a drug-like and promising chemotype that, along with the hetaryl variations, represents an alternative and thrifty tool for chemical space exploration aimed at MMP inhibitor design.     

Dynamical analysis,circuit realization,and application in pseudorandom number generators of a fractional-order laser chaotic system

A new five-dimensional fractional-order laser chaotic system (FOLCS) is constructed by incorporating complex variables and fractional calculus into a Lorentz-Haken-type laser system. Dynamical behavior of the system, circuit realization and application in pseudorandom number generators are studied. Many types of multi-stable states are discovered in the system. Interestingly, there are two types of state transition phenomena in the system, one is the chaotic state degenerates to a periodical state, and the other is the intermittent chaotic oscillation. In addition, the complexity of the system when two parameters change simultaneously is measured by the spectral entropy algorithm. Moreover, a digital circuit is design and the chaotic oscillation behaviors of the system are verified on this circuit. Finally, a pseudo-random sequence generator is designed using the FOLCS, and the statistical characteristics of the generated pseudo-random sequence are tested with the NIST-800-22. This study enriches the research on the dynamics and applications of FOLCS.     

一种新型回路电阻测试仪的研究与设计

针对传统低压回路电阻测试仪只能在被测设备停电时使用的一大限制,本文提出并设计了一种新型低压回路电阻测试仪。该仪器可在低压设备运行状态下对其回路电阻进行测量,在保证测量精度的前提下减少了设备停电率,大大提高了工作效率。     

On the performance of improved quadrature spatial modulation

Quadrature spatial modulation (QSM) utilizes the in‐phase and quadrature spatial dimensions to transmit the real and imaginary parts of a single signal symbol, respectively. The improved QSM (IQSM) transmits two signal symbols per channel use through a combination of two antennas for each of the real and imaginary parts. The main contributions of this study can be summarized as follows. First, we derive an upper bound for the error performance of the IQSM. We then design constellation sets that minimize the error performance of the IQSM for several system configurations. Second, we propose a double QSM (DQSM) that transmits the real and imaginary parts of two signal symbols through any available transmit antennas. Finally, we propose a parallel IQSM (PIQSM) that splits the antenna set into equal subsets and performs IQSM within each subset using the same two signal symbols. Simulation results demonstrate that the proposed constellations significantly outperform conventional constellations. Additionally, DQSM and PIQSM provide a performance similar to that of IQSM while requiring a smaller number of transmit antennas and outperform IQSM with the same number of transmit antennas.     

Molecular design of ambipolar redox-active molecules II: closed-shell systems

This mini-review highlights key structural features that should be taken into account when creating ambipolar redox-active closed-shell metal-free molecules. This type of compound is strongly required for the fabrication of all-organic ‘poleless’ batteries and semiconductors. The suggested strategies aimed at stabilization of both oxidized (cationic) and reduced (anionic) redox-states are based on the comprehensive analysis of the most successful structures taken from the recent publications.     

面向航空通信应用的边沿触发器教学设计

研究和分析了面向航空通信应用的边沿触发器教学设计。以边沿触发电路实现原理为核心,引导边沿触发机制的探究式学习；以航空机载网络通信为具体应用背景,引入科学研究和工程实现中实际问题,设计曼切斯特码检测系统实验；使得边沿触发器教学成为“知识再创造”的过程和创新实践的新载体,以期培养新工科背景下的独立、创新和实践精神。     

关于硬件木马电路检测技术分析及发展趋势探讨

本文结合HTH电路的复杂性等特征分析与实际应用现状,研究了HTH电路的具体检测技术方法并对当前热点技术进行对比分析,探讨了HTH电路检测方法的技术发展趋势。     

Response surface methodology toward the optimization of high-energy carotenoid extraction from Aristeus antennatus shrimp

High-energy assisted extraction techniques, like ultrasound assisted extraction (UAE) and microwave assisted extraction (MAE), are widely applied over the last years for the recovery of bioactive compounds such as carotenoids, antioxidants and phenols from foods, animals and herbal natural sources. Especially for the case of xanthophylls, the main carotenoid group of crustaceans, they can be extracted in a rapid and quantitative way with the use of UAE and MAE.     

Pure tetrahedral quadruple systems with index two

An oriented tetrahedron defined on four vertices is a set of four cyclic triples with the property that any ordered pair of vertices is contained in exactly one of the cyclic triples. A tetrahedral quadruple system of order $n$ with index $\lambda$, denoted by ${\text{TQS}}_{\lambda }\left(n\right)$, is a pair $\left(X,\mathrm{?}\right)$, where $X$ is an $n$‐set and $\mathrm{?}$ is a set of oriented tetrahedra (blocks) such that every cyclic triple on $X$ is contained in exactly $\lambda$ members of $\mathrm{?}$. A ${\text{TQS}}_{\lambda }\left(n\right)$ is pure if there do not exist two blocks with the same vertex set. When $\lambda =1$, the spectrum of a pure TQS $\left(n\right)$ has been completely determined by Ji. In this paper, we show that there exists a pure ${\text{TQS}}_2\left(n\right)$ if and only if $n\equiv 1,2\left(\mathrm{mod}3\right)$ and $n\ge 7$. A corollary is that a simple ${\text{QS}}_4\left(n\right)$ also exists if and only if $n\equiv 1,2\left(\mathrm{mod}3\right)$ and $n\ge 7$.     

以用户为中心的可见光通信协作传输中训练资源分配算法

以用户为中心的可见光通信协作传输是近年来出现的新架构,这导致虚拟小区之间出现重叠。为避免导频污染问题,每个虚拟小区中的光接入点(AP)或者虚拟小区中选择相同AP的用户发送的训练序列应该是正交的。针对可见光通信中以用户为中心的协作网络,研究训练资源的正交分配问题,提出了一种新的导频分配算法,联合导频分配和用户选择问题,以期最大限度地增加虚拟小区内可被接入的用户数。分析和仿真结果表明,该导频分配方案可以有效改善导频污染问题,提高训练资源利用率,并且相比已有的导频分配方案,性能有所改进。