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.     

Homogenization of layered elastoplastic composites: Theoretical results

Exact closed-form solutions are derived that completely characterize the effective behavior of a composite material made of elastic-perfectly plastic parallel plane layers perfectly bonded together. The derivation is framed within a rigorous theory of homogenization for elastoplastic composites, and based on the fundamental fact that the in-plane part of the strain tensor and the out-of-plane part of the stress tensor are uniform throughout the composite provided no free-edge effects occur. The obtained expressions are coordinate-free and valid in the general anisotropic case. As an example, a layered composite material with isotropic constituents is examined in detail.     

铁电体爆-电换能的实验研究

使用掺铌PZT97.5/2.5铁电陶瓷样品在垂直工作模式下,进行了爆-电换能的实验研究。在电感-电容并联负载上获得了1360安的峰值电流;在电阻负载上获得了145×10³伏的峰值电压。实验结果与理论预计符合得比较好。 关键词：     

关于GB型空间的若干结果

本文对GB型空间进行了若干讨论,得到了一些结果。 设X为Banach空间,X为X的共轭空间,B(X,X)为X到X的所有有界线性算子组成的空间。如果X中的弱收敛序列为弱收敛序列,则称X为GB型空间。Grothendieck.A于1953年证明了l~∞是GB型空间。显然自反空间是GB型空间。     

里德伯钠原子经绝热快速通道的布居数跃迁相干控制

运用含时多态展开方法和B-样条函数研究了啁啾频率微波场中里德伯钠原子的量子态之间的布居数迁移.计算了里德伯钠原子n=70-77的开普勒频率.计算了在不同的微波场中六个态的布居数从n=70到n=77随时间的迁移,布居数跃迁到最终态n=77达到了98%,这可以通过连续的单光子跃迁来实现.结果表明,通过优化微波脉冲参数可以实现从低态到较高态的布居跃迁的相干控制.     

相变及空位缺陷对高压下GeO_2光学性质的影响

本文采用第一性原理方法,在100 GPa的压力范围内,计算了GeO_2理想晶体和含锗、氧空位点缺陷晶体的光学性质.吸收谱数据表明,压力诱导的三个结构相变对GeO_2晶体的吸收谱均有影响:第一个相变将导致其吸收边蓝移,而第二和第三相变将使得其吸收边红移.锗和氧空位点缺陷的存在将导致GeO_2的吸收边红移,但氧空位点缺陷引起的红移更明显.尽管如此,分析发现,在100 GPa的压力范围内,压力、相变以及空位点缺陷等因素都不会导致GeO_2晶体在可见光区出现光吸收现象(是透明的).波长在532 nm处的折射率数据显示,在GeO_2的四个相区,其折射率均随压力增加而降低;而且,GeO_2的三个结构相变以及锗、氧空位点缺陷都会导致其折射率有所增大.本文预测,GeO_2有成为冲击光学窗口材料的可能.     

平面波超声成像中的波束合成方法研究进展

平面波成像通过单次全孔径发射-接收即可获取整幅图像,将成像帧频显著地提升至1000帧/秒以上.然而,平面波成像过程中发射的非聚焦波束将导致回波信号信噪比降低,进而使图像的分辨率和对比度变差.通过多角度相干复合成像技术可以改善平面波成像的图像质量,但是会以牺牲帧频为代价.因此研究人员们开始将新型波束合成技术引入平面波成像...     

The Dual Properties of Lk-UR and k-SS Space

In this paper, we get some properties in the dual space of Lk-UR and k-SS Banach space.AMS Subject Classification: 46B09