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.     

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.     

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．     

浙江萧山、舟山和福建集美臭鼩血红蛋白、血清蛋白电泳比较研究

本文用血红蛋白的薄层等电聚焦技术对浙江萧山、舟山和福建集美的三地臭鼩进行比较,结果显示:大陆(萧山与集美)和海岛(舟山)之间的带谱存在差异.大陆有6条区带,海岛的带谱变化较大,存在四种不同类型.用血清蛋白的SDS-聚丙烯酰胺凝胶电泳技术和血清蛋白的薄层等电聚焦技术对上述三地臭鼩的分析表明:海岛个体血清蛋白的成份和在血液中相对含量较大陆为少,而大陆萧山和集美的血清蛋白在血液中的相对含量和成份亦略有不同.     

海洋蔓足类与宿主动物的共栖关系

蔓足类的宿主动物极为广泛，自海绵动物至脊椎动物皆有代表.生活方式有无机固着生活、兼性共栖和专主共栖3种生态类群，以共栖种类占绝对优势(48.2%).蔓足类在宿主体上的定着位置与其利用水流的方式有关，其形态结构、个体大小与宿主的生物学和习性有关.蔓足类与宿主的共栖还与系统发育有关，较古老的种类主要附着在岩石或其它无机物上，与宿主共栖的种，对宿主无明显选择性;较近代的种，对宿主则有明显选择性.