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In order to obtain versatile ulitity of host molecules, three new chiral calix [4] crown ethers containing aza, thio atoms bearing two chiral sites provided by -cysteine ester were synthesized by the condensation of calix [4] arene diacid dichloride with oligoethylene glycol bridged bis-amino acid methyl ester. All new compounds were characterized by NMR, MS and elemental analysis.

以-半胱氨酸为手性源,利用多甘醇二氯醚在碱性条件下对半胱氨酸巯基进行烷基化反应,成功地合成了多甘醇醚链桥联的半胱氨酸衍生物,醚化反应后,在高度稀释条件下与对叔丁基杯[4]芳烃二乙酰氯进行双功能基缩合反应成功地合成了新型的手性杯[4]含氮、硫杂冠醚,并利用〓H NMR、MS等谱图手段对其结构进行了表征。

Bemoaned Thio Su Mien, their 71-year old matriarch.

她们71岁的女长辈黄嗣绵感叹说。

Methods: Eleven B-CLL patients were studied. Leukemic lymphocytes with (n=8) or without (n=3) P2z receptors were exposed in vitro to ATP, benzoylbenzoic-ATP, 2-methylthio-ATP(2MeSATP), adenosine-5′-[γ-thio] triphosphate, and other nucleosides for 8h. Apoptosis was detected by electron microscopy, agarose gel electrophoresis, and quantitative TdT assay. Results:Apoptosis was detected only in leukemic lymphocytes with P2z receptors. By using the quantitative assay, ATP-inducing DNA strand breaks were found to occur specifically for BzATP, ATP and 2MeSATP, but not for ATP-γS and other nucleosides.

将表达P2z受体[P2z]与不含P2z受体[P2z]的两组CLL细胞分别同1.0mmol/L三磷酸腺苷体外培养8小时,以电镜、DNA凝胶电泳和定量DNA 3′端TdT法检测细胞凋亡;并对ATP、苯甲酰苯甲酸ATP、2-甲基硫ATP(2MeSATP)、γ-硫代ATP及其它核苷的诱导效应和氧化型ATP、1-[N,O-二(5-异喹啉碘酰基)N-甲基-L-酪氨酰]-4-苯哌嗪KN-62)的抑制效应做定量研究。

Motilin and gastrin induced contraction of isolated gastric smooth muscle cells in a dose-dependent manner.(2) Motilin- and gastrin-induced antral smooth muscle cell contraction was inhibited by antibodies against Gαi-3. Motilin and gastrin caused an increase of Guanosine-5′-(3-[35S]thio)triphosphate([35S]GTPγS) binding of Gαi-3.(3) Contraction of antral muscle cells induced by motilin and gastrin was inhibited by the phospholipase C inhibitor U-73122 and the IP3 receptor antagonist heparin.

结果显示:(1)胃动素和胃泌素对胃窦平滑肌细胞均有收缩作用;(2) Gαi-3抗体可抑制胃动素和胃泌素加强胃窦平滑肌细胞的收缩,胃动素、胃泌素明显增加Gαi-3抗体与[35S]GTPγS的结合;(3)磷脂酶C抑制剂U-73122、三磷酸肌醇受体拮抗剂肝素可抑制胃动素和胃泌素引起的胃窦平滑肌细胞的收缩。

Matthews GV, Bartholomeusz A, Locarnini S, Ayres A, Sasaduesz J, Seaberg E, Cooper DA, Lewin S, Dore GJ, Thio CL.

随着治疗持续时间的延长,这种突变的流行率增加,治疗4年以上的患者达到94%。

Methods n-Cetyl-l-thio-β-D-galactoside was synthesized by a series of reaction from galactose and incorporated into Small Unilamellar Vesicles which was prepared by sonication at the ratio for L-α-PC∶Chol∶L-α-PE as 7∶2∶1, with or without 10 mol%Cetyl-gal.

半乳糖经乙酰化、溴化、缩合、亲核取代反应制备半乳糖新糖脂质并与其他脂质制备脂质体,在二氯化锡还原作用下用99mTc标记脂质体,进行动物体内靶肝实验,用γ计数器检测各脏器放射性,计算摄取率。

In this paper, the stable Au complexes are classified according to the coordination atoms and their characteristic structure. The recent development of the researches on the antitumor activity of Au complexes including the structure-activity relationship, biological targets and the mechanisms of action are reviewed. The structure of the coordination ligand and the leaving group have great impact on the in vitro cytotoxicity of the Au complex. Many physical and biological methods are introduced to study the interaction between the Au complexes and the suspected bio-target, such as DNA, protein, mitochondrion, thio-containing biomolecules, etc. The interaction modes (intercalating, electrostatic interaction, covalent bonding, etc.) are focused to illustrate the reason for the antitumor activity of Au complexes.

本文按配位原子的不同总结了稳定三价金配合物的结构特征,按其生物活性的构效关系、生物靶点和作用机制综述了三价金配合物抗肿瘤活性研究的最新成果:配体的结构特点以及离去基团对三价金配合物的体外细胞毒性影响较大;介绍了用于检测三价金配合物与可能的生物靶分子之间的相互作用的多种物理和生物学方法,重点关注了相互作用的模式,如嵌入/静电吸引/共价结合等,并解释了三价金配合物抗肿瘤活性的原因。

In this paper, the stable Au complexes are classified according to the coordination atoms and their structural characteristics. The recent development of the researches on the antitumor activity of Au complexes including the structure-activity relationships, biological targets and the mechanisms of action are reviewed. The structure of the coordination ligand and the leaving group have great impact on the in vitro cytotoxicity of the Au complex. Many physical and biological methods are introduced to study the interaction between the Au complexe and the suspected bio-target, such as DNA, protein, mitochondrion, thio-containing biomolecules, etc. The interaction modes (intercalating, electrostatic interaction, covalent bonding, etc.) are focused to illustrate the reason for the antitumor activity of Au complexes.

本文按配位原子的不同总结了稳定三价金配合物的结构特征,按其生物活性的构效关系、生物靶点和作用机制综述了三价金配合物抗肿瘤活性研究的最新成果:配体的结构特点以及离去基团对三价金配合物的体外细胞毒性影响较大;介绍了用于检测三价金配合物与可能的生物靶分子之间相互作用的多种物理和生物学方法,重点关注了相互作用的模式,如嵌入/静电吸引/共价结合等,并解释了三价金配合物抗肿瘤活性的原因。

The thiopeptides, by binding within a cleft located between the ribosomal protein L11 and helices 43 and 44 of the 23S rRNA, overlap with the position of domain V of EF-G, thus explaining how this class of drugs perturbs translation factor binding to the ribosome.

核糖体蛋白L11和23SrRNA的43/44螺旋结构形成裂隙,L11的构象变化能够加宽该裂隙从而允许延伸因子EF-G插入,促使GTP水解,为肽链延伸合成过程中核糖体的构象变化提供能量,而Thio能够与L11和23sRNA结合,阻止L11的构象变化,使该裂隙处于闭合状态,抑制EF-G在延伸过程中的作用。

Their extraction properties have been studied by metal picrates liquid-liquid extraction and the results show:By using three thio-heterocyclic compounds, twelve novel derivatives of thioalkoxycalix[4]arenes on the lower rim have been synthesized and structurally characterized by 1H NMR、13C NMR、IR and MS.

本文采用三种巯基杂环化合物对杯芳烃下沿进行修饰,得到了下沿含有杂环硫烷氧基的杯芳烃系类系列衍生物,并利用~1H NMR、~(13)C NMR、IR和MS对所合成的十二个未见文献报道的新化合物进行了结构表征。

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Since this year, in a lot of villages of Beijing, TV of elevator liquid crystal was removed.

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