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1.
《Arabian Journal of Chemistry》2022,15(1):103492
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. 相似文献
2.
Yujie Chen Yiping Song Zhen Zhang Yali Chen Qiliang Deng Shuo Wang 《Advanced functional materials》2021,31(41):2104885
Various products, including foods and pharmaceuticals, are sensitive to temperature fluctuations. Thus, temperature monitoring during production, transportation, and storage is critical. Facile indicators are required to monitor temperature conditions via color changes in real time. This study aimed to prepare and apply thiol-functionalized covalent organic frameworks (COFs) as a novel indicator for monitoring thermal history and temperature abuse. The COFs underwent obvious color changes from bright yellow to purple after exposure to different temperatures for varying durations. The reaction kinetics are analyzed under isothermal conditions, which reveal that the order of reaction rates is k−20°C < k4°C < k20°C < k35°C < k55°C. The activation energy (Ea) of the COFs is calculated using the Arrhenius equation as 50.71 kJ moL−1. The COFs are capable of sensitive color changes and offer a broad temperature tracking range, thereby demonstrating their application potential for the monitoring of temperature and time exposure history during production, transportation, and storage. This excellent performance thermal history indicator also shows promise for expanding the application field of COFs. 相似文献
3.
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. 相似文献
4.
乳腺疾病已严重危害女性身心健康,其中乳腺癌更位居全球范围内女性癌症发病率和死亡率首位,因此乳腺癌的早期发现意义重大。传统结构影像学早期检测疾病具有一定局限性,而红外热成像作为功能成像技术可为乳腺癌的早期筛查提供有效线索。因此本文主要就红外热成像在乳腺疾病的早期检测及预后评估的应用价值进行综述。 相似文献
5.
Vyacheslav V. Sentyurin Oleg A. Levitskiy Tatiana V. Magdesieva 《Current Opinion in Electrochemistry》2020
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. 相似文献
6.
7.
Thalia Tsiaka Panagiotis Zoumpoulakis Vassilia J. Sinanoglou Constantinos Makris Georgios A. Heropoulos Antony C. Calokerinos 《Analytica chimica acta》2015
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. 相似文献
8.
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 with index , denoted by , is a pair , where is an ‐set and is a set of oriented tetrahedra (blocks) such that every cyclic triple on is contained in exactly members of . A is pure if there do not exist two blocks with the same vertex set. When , the spectrum of a pure TQS has been completely determined by Ji. In this paper, we show that there exists a pure if and only if and . A corollary is that a simple also exists if and only if and . 相似文献
9.
Vito Gigante Laura Aliotta Maria Beatrice Coltelli Patrizia Cinelli Luigi Botta Francesco Paolo La Mantia Andrea Lazzeri 《Journal of polymer science. Part A, Polymer chemistry》2020,58(23):3264-3282
The development of biodegradable materials for tailored applications, particularly in the field of polymeric films and sheets, is a challenging technological goal as well as a contribution to help protect the environment. Poly(lactic) acid (PLA) is a promising substitute for several oil-based polymers; however, to overcome its thermal and mechanical drawbacks, researchers have developed solutions such as blending PLA with polybutylene adipate terephthalate (PBAT), which is capable of increasing the ductility of the final material. In this study, PLA/PBAT binary blends, with minimum possible content of nonrenewable materials, were examined from processing, thermal, morphological, and rheological perspective. An optimized PLA/PBAT ratio was chosen as the polymeric basis to obtain a biodegradable formulation by adding a biobased plasticizer and appropriate fillers to produce a micrometer film with tailored flexibility and tear resistance. The processing technology involved flat-die extrusion, followed by calendering. The tearing resistance of the produced film was investigated, and the results were compared with literature data. A study on the essential work of fracture was implemented to explore the mode III out-of-plane fracture resistance starting from a trouser tear test. 相似文献
10.
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。 相似文献