Synthesis of 4-（2-Phenylhydrazono）-l-（4-phenylthiazol-2-yl）- 1H-pyrazol-5（4H）-one Compounds and Characterization of Their Affinities to Anti-apoptotic Bcl-2 Family Proteins

Organic compounds containing the thiazol-2-yl-lH-pyrazol-5（4H）-one moiety are known to be associated with versatile pharmacological applications. In this study, we describe the methods for preparing 4-（2-phenylhydrazono）- l-（4-phenylthiazol-2-yl）-1H-pyrazol-5（4H）-one compounds. A set of 26 compounds were synthesized with overall yields ranging between 37%-92%. They were tested in a fluorescence polarization-based binding assay against three anti-apoptotic Bcl-2 family proteins, including Bcl-xL, Bcl-2, and Mcl-1. Our results indicate that this class of compounds are not effective inhibitors of these anti-apoptotic Bcl-2 family proteins. Their apoptosis-inducing ef- fects are possibly due to BAX activation as suggested by Gavathiotis et al. in their recent study. However, other possibilities should not be ignored. In addition, a crystal structure obtained by us reveals that the exocyclic double bond in the molecular structure of this class of compounds is in the （Z）-configuration.     

有机物结构诱导剂调控WO3晶体晶面的研究进展

太阳能半导体光催化技术由于其绿色无污染、可再生,有利于解决全球变暖问题等优点而受到国内外研究人员的广泛研究。由于半导体光催化剂的催化活性取决于其表面电子结构和原子结构,而这些结构又强烈地依赖于晶体层面,因此光催化剂的催化活性受到反应过程中暴露的晶面的显著影响。近年来,晶面调控工程已成为一种非常重要的半导体理化性质微调方法。三氧化钨(WO₃)半导体催化剂由于具有较好的光催化性能,常用作光电催化系统中的光阳极。本文针对目前国内外使用有机物(有机小分子及有机大分子)作为结构诱导剂对WO₃晶面调控的研究现状进行了综述,分析有机物对晶体晶面调控的规律和原理,寻找新的实验方向以及突破点,总结目前WO₃光电催化在实际生产生活中的应用,例如光电催化分解水、电致变色、气体传感器、有机污染物降解等,并对未来实验发展方向进行展望。     

A novel approach toward the synthesis of strigolactones through intramolecular [2+2] cycloaddition of ketenes and ketene-iminiums to olefins. Application to the asymmetric synthesis of GR-24

An intramolecular [2+2] cycloaddition of ketenes and ketene-iminium was developed for the preparation of GR-24, a synthetic analogue of the family of strigolactone plant hormones. Excellent levels of regioselectivity and of chiral induction were obtained using a bulky chiral amine for the formation of the cyclobutanone and a subsequent regioselective Baeyer-Villiger afforded the tricyclic lactone core of (+)-GR-24.     

EMMPRIN磷酸化突变质粒的构建及功能检测

利用聚合酶链式反应(PCR)定点诱变技术,对细胞外基质金属蛋白酶诱导因子(EMMPRIN)的2个磷酸化位点进行突变,构建了EMMPRIN磷酸化位点突变质粒.对其功能进行检测发现,EMMPRIN磷酸化位点突变质粒可在细胞内正常表达.研究结果显示,突变质粒可抑制肿瘤细胞的增殖(P<0.05),表明EMMPRIN可能与肿瘤细胞的增殖相关.     

Light‐Induced Protein Dimerization by One‐ and Two‐Photon Activation of Gibberellic Acid Derivatives in Living Cells

We developed a highly efficient system for light‐induced protein dimerization in live cells using photo‐caged derivatives of the phytohormone gibberellic acid (GA₃). We demonstrate the application of the photo‐activatable chemical inducer of dimerization (CID) for the control of protein translocation with high spatiotemporal precision using light as an external trigger. Furthermore, we present a new two‐photon (2P)‐sensitive caging group, whose exceptionally high two‐photon cross section allows the use of infrared light to efficiently unleash the active GA₃ for inducing protein dimerization in living cells.     

Synthesis and photochromic properties of WO<Subscript>3</Subscript> powder induced by oxalic acid

Tungsten trioxide powder with the novel morphology was prepared via the hydrothermal method with oxalic acid as the organic inducer, the structure and shape of which were detected by X-ray diffraction (XRD), scanning electron microscopy (SEM) and BET. Furthermore, photochromic properties of the as-prepared powder samples were tested by an ultraviolet-visible spectrophotometer combined with a color difference meter. The corresponding results indicated that the induced product was still hexagonal WO₃, made up of regularly spindle particles with 200–300 nm in length and 30–50 nm in width. The ratio of the length and width was from 4 to 10. Moreover, the special morphology improved its absorptive capacity to the excitation light source, resulting in its high photochromic properties. Supported by the National Natural Science Foundation of China (Grant No. 50702052) and the Hubei Province Key Laboratory of Macromolecular Material     

3-Aza-8,10-dioxa-bicyclo[5.2.1]decane (9-exo BTKa) carboxylic acid as a new reverse turn inducer: synthesis and conformational analysis of a model peptide

Dipeptide isostere 5, belonging to the class of 9-exo BTKa, was synthesised starting from R,R-tartaric acid and 4-nitro-1-(3-nitrophenyl)butan-1-one. The nine-membered lactam showed interesting structural features and was inserted in a 5-residue model peptide. The conformational properties of this modified peptide have been studied by NMR and molecular modelling, indicating that compound 5 acted as a reverse turn inducer.     

高速离心泵串联诱导轮的设计理论及工程实现

阐述了高速离心泵串联诱导轮的设计理论及工程实现,提出了第一级诱导轮采用变螺距结构而第二级诱导轮采用锥形等螺距结构的设计方案。经过理论分析、试验研究和工程应用表明,串联诱导轮可使高速泵获得比带单级诱导轮更高的汽蚀性能。