3-取代-12-氧代-N,N-双(2-氯乙基)脱氧胆酰胺的合成及其抑制癌细胞活性

以7-脱氧胆酸(1)为原料,由Jones试剂氧化得到3,12-二氧代-7-脱氧胆酸(2),然后与双(2-氯乙基)胺反应,得到3,12-二氧代-N,N-双(2-氯乙基)-7-脱氧胆酰胺(4),进一步通过对化合物4中的3-位羰基进行官能团转换,得到2个3-位分别被肟基、缩胺硫腙基取代的12-氧代-N,N-双(2-氯乙基)-7-脱氧胆酰胺类型化合物。同时,初步测试了合成物对肿瘤细胞增殖抑制活性,结果表明,化合物对宫颈癌细胞的生长有显著的抑制活性。     

Copper(II) catalyzed cross-dehydrogenative coupling of cyclic benzylic ethers with simple carbonyl compounds by Na2S2O8

Copper(II) catalyzed cross-dehydrogenative coupling of cyclic benzylic ethers with a variety of simple carbonyl compounds mediated by Na₂S₂O₈ is developed. The scope of carbonyl components is broad, including simple aldehydes as well as ketones. The use of Na₂S₂O₈ as the oxidant for the CDC reaction is attractive based on economical and environmental factors.     

具有特殊甾核结构甾体化合物的合成及生理活性研究进展

改变甾体的甾核结构,在甾核或支链中引入不同的官能团,可以得到一些具有不同生理活性的化合物.按照不同类型甾核结构分类,结合本课题组在具有特殊甾核结构甾体化合物的合成和生理活性研究方面所取得的一些成果,对近年来具有A-失碳甾体化合物、B-失碳甾体化合物及C-失碳-D-增碳甾体化合物的合成及生理活性进行讨论,并展望了此类化合物的发展趋势及应用前景.     

GaAs pyramidal quantum dot coupled to wetting layer in an AlGaAs matrix: A strain-free system

In this contribution, the electronic and linear and nonlinear optical properties of pyramid-shaped GaAs quantum dots (QDs) coupled to wetting layer (WL) in an Al_0.3Ga_0.7As matrix have been investigated. This nanostructure is relaxed from strain effects due to very small lattice-mismatching. Three transitions of P-to-S, WL-to-P, and WL-to-S were considered and the corresponding transition dipole moments, oscillator strengths, and linear and nonlinear optical properties regarding to these transitions were investigated as a function of the QD height. The results showed that for P-to-S transition, which is a purely in-plane-polarized transition, the dependence of electronic and optical properties on the size is moderate and can be neglected. But for WL-to-P and WL-to-S transitions, which are in-plane- and z-polarized transitions, respectively, the electronic as well as optical properties are strongly size-dependent. Furthermore, a competition between WL-to-S and WL-to-P transitions was observed when the QD size changed.     

Aharonov–Bohm effect in non-uniform crater-like quantum dot with double rim

We study electron energies in a double concentric quantum ring with anisotropy in the rims heights in the presence of the external magnetic field applied along the symmetry axis. To this end, we consider a model in which the thickness grows linearly from the axis up to the inner rim with a slope different from one between the inner and the outer rims. The anisotropy in the rims heights originated by the presence in the structure of various valleys we simulate by periodic dependence of the slope on the radial direction. We show that the wave functions of the electron confined in such structure can be found analytically if the slopes in all radial directions are the same, and by using a simple exact diagonalization procedure otherwise. The behavior of the electron energies as functions of the magnetic field, rings radii and rims heights, as well as the number of the valleys and their depths is consistently described with our formalism. The entanglement of the states with different radial and orbital quantum numbers, the period and the amplitude of the Aharonov–Bohm oscillations are very sensible to any variations of the rims heights.     

2-甲酰噻吩缩氨基硫脲及其芳基钌配合物的合成、结构与抗癌活性研究

合成了2-甲酰噻吩缩氨基硫脲化合物L1,L2和它们的芳基钌配合物[(η6-p-cymene)RuII(TSC)Cl]Cl(1:TSC=L1,2:TSC=L2),其结构经1H NMR,MS和元素分析确认.通过单晶培养得到了1的晶体,并测定其晶体结构.凝胶电泳实验表明,L1和L2与1和2对pBR322质粒DNA存在不同的作用机理.采用MTT法测定了这些化合物对3种人体肿瘤细胞株(SGC7901,BEL7404和CNE-1)的细胞毒活性.其中化合物1对人鼻咽癌细胞株(CNE-1)的有较好的抑制活性,其IC50值为27.8μmol L-1.     

一种具有抗肿瘤活性胆酸衍生物的合成新方法

以胆酸为原料, 使之与甲醇反应, 得到胆酸甲酯(2). 2采用PCC(氯铬酸吡啶)氧化得到脱氢胆酸甲酯(3), 3在CoCl2存在的条件下通过NaBH4的化学选择性还原得到7α-羟基-3,12-二氧代胆酸甲酯(4). 对4的抗肿瘤活性试验表明该化合物对Sk-Hep-1(肝癌)和H-292(肺癌)细胞株具有中等程度的细胞毒性.     

多羰基甾酮的选择性还原反应研究

在不同金属离子存在下,多羰基甾酮的甾核及支链上都发生了羰基与硼氢化钠的还原反应,得到具有不同的区域选择性和立体选择性的还原产物.