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.     

Synthesis of tetrasubstituted thiophenes from pyridinium 1,4-zwitterionic thiolates and modified activated alkynes

Pyridinium 1,4-zwitterionic thiolates were applied to a formal [3 + 2] annulation reaction with modified activated alkynes, affording various tetrasubstituted thiophenes with aryl, alkenyl, alkyl or silyl group at the special position. The structural modification of alkyne substrates enabled the synthesis of diverse thiophenes to be achieved using the pyridinium 1,4-zwitterionic thiolates as the sulfur-containing building blocks. This approach is metal-free and catalyst-free.     

D形光纤Bragg光栅弯曲灵敏度的理论和实验研究

用材料力学理论分析了D形光纤Bragg光栅（D-shaped fiber Bragg grating,D-FBG）以及常规光纤Bragg光栅由弯曲引起的轴向应变,得到了光栅Bragg波长漂移的弯曲敏感特性.实验结果和理论计算结果基本相符.与常规FBG相比,该D-FBG的弯曲灵敏度要高近80倍.因此D-FBG可以直接应用于弯曲形变的测量,以及间接应用于压力、加速度等物理量的测量.理论分析和实验结果对采用该类型光纤光栅的器件和传感系统的设计具有参考意义.     

光学变换中的离散取样方法

本文研究了光学变换中的离散取样问题。基于幺正变换的考虑,求得了光学变换中离散取样方法所依据的条件。导出了包含取样单元透光孔作用的光传播矩阵。最后,以自然序Walsh变换为例,具体计算了变换所需全息透镜的振幅与相位分布及相应的误差。 关键词：     

Quadrupole interaction in In0.95 Ag0.045 Ga0.005 alloy

The temperature dependence of the quadrupole interaction of¹¹¹Cd in the In_0.95 Ag_0.045 Ga_0.005 alloy is determined by the time differential perturbed angular correlation method from 77 to 422 K. The electric field gradients produced by the lattice are derived. The temperature dependence of the electric field gradient is found to follow theT ^3/2 law observed in In between 77 K and room temperature and to deviate from it at higher temperatures. The widths of the electric field gradient distribution are 0.1147(259), 0.0924(340), 0.4954(601) and 1.344(175) at 77, 298, 373 and 422 K, respectively. This illustrates that the alloy is well ordered at 77 and 298 K and that it becomes less ordered at 373 and 422 K.     

一组新型络合物晶体结构与光学性能的研究

研究了二氯三烯丙基硫脲合镉(ATCC),二氯三烯丙基硫脲合汞(ATMC)和二溴三烯丙基硫脲合镉(ATCB)三种晶体的结构特点.首次报道了ATMC和ATCB晶体的非线性光学系数及倍频性能;文中分析比较了三种晶体的非线性光学性能;讨论了晶体结构与性能的关系,为探索高效非线性光学新材料提供依据.     

一种动态实时的遥感专题应用系统定制框架

遥感专题应用系统广泛用于遥感影像的加载、分析、专题提取、出图等.为实现遥感专题应用系统动态、实时和可扩展的定制化开发,设计了一套基于组件的遥感专题应用系统定制框架：定义了组件划分方式,将专题系统划分为功能类组件和容器类组件,建立了组件属性和组件间的关系;采用XML文件描述遥感专题应用系统中的组件,并提供从XML到遥感专题应用系统的解析方法;设计了遥感专题应用系统定制平台,提出一种动态实时的软件设计方法,可以“所见即所得”地定制遥感专题应用系统,并将其保存为XML文件.采用该定制平台定制的多个专题系统已应用于相关部门.该框架为快速高效定制遥感专题应用系统提供了一种新的开发设计模式,降低了遥感数据在多行业应用的技术门槛,减少重复性开发工作.     

螯合树脂研究──ⅩⅩⅦ·巯基胺型螯合树脂的化学改性及其吸附性能

巯基胺型螯合树脂经烷氧基环硫丙烷和二烷基胺基环硫丙烷改性后。合成了一系列新的螫合树脂．这些树脂与原树脂相比，对贵金属离子的吸附性能有一定的改善．特别是用二烷基胺基环硫丙烷改性后的树脂，效果更为明显．还讨论了树脂结构与吸附性能之间的关系．     

近江牡蛎受精细胞学研究

用醋酸──地衣红染色的方法对近江牡蛎人工授精的卵子减数分裂和受精过程进行了详细的细胞学观察．精子入卵前，卵子处于第一次减数分裂的前期（胚泡期），精子入卵后，胚泡消失，然后进行两次减数分裂，在海水温度为２８．８℃的情况下，授精后３３ｍｉｎ和４５ｍｉｎ，绝大部分受精卵已排出第一极体和第二极体，雄原核可在第一极体排出后及第二极体排出前任何时期内形成，雌雄原核以联合的方式将两组染色体合并，授精后１ｈ，大部分卵子完成第一次卵裂．在２５℃和２６℃授精的情况下，观察到了较多的多精入卵的现象．卵子发育的非同步性现象非常明显．