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111.
Dr. Zhaojun J. Sheng Dr. Yiming M. Shi Ximing Xu Sébastien Bellynck Kun Zhang Prof. Zhiyun Y. Du Xuetao Xu Prof. François Maurel Prof. Chang-Zhi Dong 《ChemistryOpen》2019,8(1):34-40
In order to develop original water soluble antagonists of X-linked inhibitor of apoptosis protein (XIAP), a novel bicyclic scaffold was designed based on 8,5-fused bicyclic lactam. During its preparation, a spontaneous rearrangement from 8,5- to 7,5-fused bicyclic lactam was observed and confirmed by MS and NMR analyses, in particular the HMBC spectra. DFT calculations were performed to understand the corresponding mechanism. It was finally prevented through changing the reaction order in the synthesis route and a Smac mimetic with this core structure, ZJ-1 was successfully obtained. The structure of this new bicyclic scaffold was well confirmed by HRMS and NMR (1H, 13C, NOESY) analyses. ZJ-1 presented in addition a binding affinity to XIAP-BIR3, nearly 6 times better than that of AVPI, similar to the reported SM-128 in an in vitro fluorescence polarization (FP) assay. This preliminary result suggests that this new bicyclic scaffold could be very attractive in the development of novel anticancer agents targeting XIAP. 相似文献
112.
Weina Zhang Zhongbing Huang Ximing Pu Xianchun Chen Guangfu Yin Lei Wang Fei Zhang Fabao Gao 《中国化学快报》2020,31(1):285-291
It is urgent to find a technology accurately to better diagnose and treat to brain tumor.Eu-doped Gd2 O3 nanorods(Eu-Gd2 O3 NRs)with paramagnetic and fluorescent properties were conjugated with doxorubicin(Dox)and chlorotoxin(CTX)via PEGylation,hydrazone bond and sulfur bond(named as CTXNRs-Dox),and these NRs could release more Dox in lower pH environment.The results of cell experiments indicated that CTX-NRs-Dox had obvious targeting and toxic effects on U251 cells,as well as good fluorescence imaging behavior.The orthotopic glioma-transplanted mice models were constructed via the intracranial injection of glioma cells(U87 MG).The result of experiments after the tail-vein injection of the prepared NRs suggested that CTX-NRs-Dox could target to brain tumors via the long-time blood circulation,leading to their obvious contrast enhancement of MR imaging of the intracranial tumor and their significant inhibitory effect on the growth and metastasis of brain tumors.A mechanism of synergistic effect of CTX-NRs-Dox on targeting and inhabiting the brain tumor was proposed.Our research suggested that CTX-NRs-Dox had potential application prospect in the detection and treatment of glioma. 相似文献
113.
Meihui Li Jianping Xu Ximing Chen Xiaosong Zhang Yanyu Wu Ping Li Xiping Niu Chengyuan Luo Lan Li 《Superlattices and Microstructures》2012
Zn1−xCoxO nanocrystals with nominal Co doping concentrations of x = 0–0.1 were synthesized through a simple solution route followed by a calcining process. The doping effects on the structural, morphological and optical properties were investigated by means of X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Raman, absorption and luminescence spectroscopy. The results indicated that a small amount of Co ions were incorporated into ZnO lattice structure, whereas the secondary phase of Co3O4 was segregated and precipitated at high Co doping concentrations, the solid solubility of Co ions in ZnO nanocrystals could be lower than 0.05. The spectra related to transitions within the tetrahedral Co2+ ions in the ZnO host crystal were observed in absorption and luminescence spectra. 相似文献
114.
We present an image recognition method to distinguish targets with cat-eye effect from the dynamic background based on target shape and modulation frequency.Original image sequences to be processed are acquired through an imaging mechanism that utilizes a pulsed laser as active illuminator and an industrial camera as detection device.There are two criterions to recognize a target: one exploits shape priors and the other is the active illuminator’s modulation frequency.The feasibility of the proposed method and its superiority over the single criterion method have been demonstrated by practical experiments. 相似文献
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117.
分析了傍轴非均匀振幅分布会聚球面波的焦移问题,给出焦移量的解析表达式,并由此进一步揭示出,导致焦移的主要原因于光束的内禀运动。 相似文献
118.
光束截面的能量守恒及能量衍射发散度 总被引:1,自引:0,他引:1
证明了任何一个在真空中稳态传输的单色标量光束,在忽略了瞬逝波的条件下,其光束截面能量的径向分量E及轴向定量E都与轴坐标无关,它们都为不变量,文中还进一步给出了光束能量衍射分散度的X,Y分量的表达式。 相似文献
119.
Synthesis and Self‐Assembly of Thermoresponsive Amphiphilic Biodegradable Polypeptide/Poly(ethyl ethylene phosphate) Block Copolymers
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Qiuhua Wu Dan Zhou Renyu Kang Xiuping Tang Qi Yang Ximing Song Guolin Zhang 《化学:亚洲杂志》2014,9(10):2850-2858
We report the design and synthesis of new fully biodegradable thermoresponsive amphiphilic poly(γ‐benzyl L ‐glutamate)/poly(ethyl ethylene phosphate) (PBLG‐b‐PEEP) block copolymers by ring‐opening polymerization of N‐carboxy‐γ‐benzyl L ‐glutamate anhydride (BLG? NCA) with amine‐terminated poly(ethyl ethylene phosphate) (H2N? PEEP) as a macroinitiator. The fluorescence technique demonstrated that the block copolymers could form micelles composed of a hydrophobic core and a hydrophilic shell in aqueous solution. The morphology of the micelles as determined by transmission electron microscopy (TEM) was spherical. The size and critical micelle concentration (CMC) values of the micelles showed a decreasing trend as the PBLG segment increased. However, UV/Vis measurements showed that these block copolymers exhibited a reproducible temperature‐responsive behavior with a lower critical solution temperature (LCST) that could be tuned by the block composition and the concentration. 相似文献
120.
Simultaneous determination of three chloroacetic acids,three herbicides,and 12 anions in water by ion chromatography
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An ion chromatography method was developed for the simultaneous detection of three soluble herbicides (glyphosate, bentazone and picloram), three chlorine disinfection byproducts (monochloroacetic acid, dichloroacetic acid and trichloroacetic acid) and 12 anions in water (Cl–, Br–, SO42–, CO32–, ClO3–, ClO4–, BrO3–, PO43–, NO2–, NO3–, CH3COO– and COO–). High linearity (r2 > 0.996) was observed for all target analytes for each respective concentration range. The limit of detection and limit of quantitation were between 0.21–0.85 and 0.06–25.46 μg/L, respectively. However, the interference effect of Cl–, NO3–, SO42– and CO32– on some target analytes must be considered during the analysis. Sample pre‐treatment by a hydrogen column (H‐column) required to reduce the negative effect of CO32–. Additionally, sample pre‐treatment by a sliver–hydrogen column (Ag–H‐column) is required when Cl– > 100 mg/L and SO42– < 50 mg/L, and pre‐treatment by both a barium column (Ba‐column) and an H‐column is required when Cl– > 100 mg/L and SO42– > 50 mg/L. When Cl– > 100 mg/L, SO42– > 50 mg/L and CO32– > 20 mg/L, the sample pre‐treatment by either an Ag–H–Ba‐column or an Ag–H‐column and Ba‐column is required to minimize interference. 相似文献