Biological evaluation of novel selenazole‐based compounds as potential thioredoxin reductase inhibitors

Recently, thioredoxin reductase as a target for treatment of tumors has attracted the attention of scientists. 1,2‐[Bis(1,2‐benzisoselenazolone‐3(2 H)‐ketone)]ethane (ethaselen, BBSKE, PCT: CN02/00412), designed and synthesized previously, is an effective thioredoxin reductase inhibitor; presently it is in phase II clinical trials, targeting gastric cancer, lung cancer and colon cancer. To seek more novel and effective anticancer drugs, we have developed many selenazole‐based compounds. Evaluation of the thioredoxin reductase inhibitory effect and investigation of the mechanism of anticancer drugs require abundant thioredoxin reductase, but since commercial thioredoxin reductase is expensive its use is often limited. Therefore, the preparation of thioredoxin reductase is necessary. Base on the above investigation, in this work we have prepared thioredoxin reductase and evaluated selenazole‐based compounds, and found that 44 compounds have high inhibitory effect on thioredoxin reductase with IC₅₀ < 10 µ m , of which 16 compounds have IC₅₀ values below 1 µ m . This is helpful in investigating and elucidating the mechanism of this kind of compound. Copyright © 2012 John Wiley & Sons, Ltd.     

Application of alkoxide in catalytic transfer hydrogenation of unsaturated nitrogen compounds

Alcoholate was utilized in catalytic transfer hydrogenation of unsaturated nitrogen compounds. In the reduction of nitro compounds, oximes and imines, alkoxide was used as the promoter, with alcohol as the hydrogen source, while in the reduction of nitriles, alkoxide was used as the hydrogen source.     

基于开放获取的黄山地方特色文献资源建设

以具有黄山地方特色的电子图书、古籍和地方志文献资源为例,对基于开放获取的黄山地方特色文献资源建设进行了探讨。     

基于物联网的矿井通风机监控系统研究

针对当前矿井通风机监控系统功能单一、反馈控制能力差能等特点,提出一种基于物联网的矿井通风机监控系统。该系统利用传感器、Wi Fi技术实现监控系统实时数据传输和反馈报警控制功能。详细描述了矿井通风机监控系统构成及各硬件设计原理图,介绍了系统的底层驱动设计及软件设计流程。通过实验证明该矿井通风机监控系统能实时传输数据,视频监控稳定,能实现报警控制,可在移动平台或者PC机上进行监控,具有一定的推广价值。     

一种高效率的四脊喇叭馈源

以天线口径效率为目标,研究了四脊喇叭口径对馈源波束等化、波束宽度恒定和天线口径效率等性能的影响,得到了一种3∶1带宽高效率圆四脊喇叭馈源的设计。该馈源在整个频带内具有较低的电压驻波比,三个主平面的主极化方向图波束等化较好,-10d B波束宽度基本恒定,且天线口径效率达到55%以上。     

Index Abstracts

Abstract

Calorimetric titrations have been performed in anhydrous acetonitrile at 25°C to give the complex stability constants (K _s) and the thermodynamic parameters (ΔGΔ, ΔHΔ and ΔSΔ) for the complexation of light lanthanoid(III) nitrates (La-Gd) with N-benzylaza-21-crown-7 3. Data analyses, assuming 1:1 stoichiometry, were successfully applied to all light lanthanoid-azacrown ether combinations employed. Using the present and previous data on 15- to 21- membered N-benzylazacrown ethers 1–3, the effect of ring size upon complexation behavior was discussed comparatively and globally from the thermodynamic point of view. The complexation behaviors are analyzed in terms of the size-fit concept, N-substituent coordination numbers, and lanthanoid's surface charge density. Thermodynamically the complexation of light lanthanoids with azacrown ethers is enthalpy-driven, while the cation selectivity is generally entropy-driven in acetonitrile.