New sorafenib derivatives: synthesis, antiproliferative activity against tumour cell lines and antimetabolic evaluation

Sorafenib is a relatively new cytostatic drug approved for the treatment of renal cell and hepatocellular carcinoma. In this report we describe the synthesis of sorafenib derivatives 4a-e which differ from sorafenib in their amide part. A 4-step synthetic pathway includes preparation of 4-chloropyridine-2-carbonyl chloride hydrochloride (1), 4-chloro-pyridine-2-carboxamides 2a-e, 4-(4-aminophenoxy)-pyridine-2-carboxamides 3a-e and the target compounds 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-phenoxy]-pyridine-2-carboxamides 4a-e. All compounds were fully chemically characterized and evaluated for their cytostatic activity against a panel of carcinoma, lymphoma and leukemia tumour cell lines. In addition, their antimetabolic potential was investigated as well. The most prominent antiproliferative activity was obtained for compounds 4a-e (IC(50) = 1-4.3 μmol·L-1). Their potency was comparable to the potency of sorafenib, or even better. The compounds inhibited DNA, RNA and protein synthesis to a similar extent and did not discriminate between tumour cell lines and primary fibroblasts in terms of their anti-proliferative activity.     

导数光谱法测定原子簇化合物中硫

本文用导数光谱法通过测定CrO_4~(2-)的含量,间接测定钼铁硫原子簇化合物中硫含量。用紫外一阶导数光谱来消除测定中干扰,免除了化学法消除干扰的麻烦。该方法测硫回收率为100±4％,精密度为4.0％。     

Determination of trace amounts of some metals in samples with high salt content by atomic absorption spectrometry after cobalt-diethyldithiocarbamate coprecipitation

A method for determination of trace amounts of Cu, Fe, Pb, Mn, Zn, Cd, Ni, Bi and Cr in aqueous solutions by flame atomic absorption spectrometry after coprecipitation by using a combination of sodium diethyldithiocarbamate as a chelating agent and cobalt as a carrier element was introduced. Different factors including amounts of reagents, pH of sample solution, standing time, sample volume for the precipitation and matrix effects were examined. Under selected conditions, the relative standard deviation of the combined method of sample treatment, coprecipitation and determination with flame AAS (n = 9) is generally about 3.5-6.9%; the limits of detection (3 s, n = 20) for the analytes were found to be between 4 and 64 microg 1(-1). The procedure was applied to the analysis of sea water and dialysis concentrate samples with quantitative recovery, > or =95%.     

Spectrophotometric determination of trace amounts of tungsten in geological samples after preconcentration on Amberlite XAD-1180

A method for the preconcentration of trace amounts of tungsten as its thiocyanate complex, using a column filled with Amberlite XAD-1180 resin, is proposed. After elution with a small volume of acetone, the analyte was determined spectrophotometrically with potassium thiocyanate and stannous chloride. The influence of several ions, as interferents, is discussed. The proposed method was applied to the determination of tungsten in geological samples with good analytical results, such as recoveries of 95% or above, relative standard deviations of 6% or below (n = 10) and a detection limit of 12 mugl(-1).     

氯苯甲酸钠在DMF-水混合溶剂中的体积性质研究

DMF是分子间没有氢键形成的分子量最小的酰胺[1],在化学、化工领域应用广泛．本文对苯甲酸钠及o－,m－,p-氯苯甲酸钠在DMF-水混合溶剂中的体积性质进行研究,讨论了溶剂效应和取代基效应对溶质-溶剂相互作用的影响．1实验部分1．1试剂苯甲酸及NaOH为分析纯试剂;o－,m－,p-氯苯甲酸（分析纯）均经乙醇一水重结晶,干燥后备从DMF为分析纯;水为二次重蒸水．对应钠盐溶液按文献［2」方法配制,其它溶液由此溶液逐级稀释而成．DMF一水混合溶剂用称量法配制,DMF的质量分数为10％～80％．1．2仪器混合物密度用AntonPaarDMA55型精…     

Interfacial enzyme activation, non-lamellar phase formation and membrane fusion. Is there a conducting thread?

Previous studies from this laboratory have shown that the enzymic generation of diacylglycerol in bilayers by phospholipase C may lead to membrane fusion through the formation of transient non-lamellar lipidic intermediates. The present paper intends to explore the correlations existing among the three main processes involved, namely (a) the induction (or inhibition) of lamellar-to-non-lamellar phase transitions in lipid mixtures through the addition of small (< 5 mol%) proportions of other lipids, (b) the promotion, by the latter lipids, of fusion in otherwise stable phospholipid vesicles (large unilamellar liposomes) under conditions leading to inverted hexagonal/inverted cubic phase formation in bulk lipid systems, and (c) the modulation, by the same small proportions of lipids, of phospholipase C hydrolysis of phosphatidylcholine in liposome bilayers. It is concluded that phospholipase C may give rise to non-lamellar lipidic structures that in turn permit liposomal fusion to occur, but neither enzyme activity is directly modulated by non-lamellar phase formation, nor will whatever kind of enzyme-induced non-lamellar structure give rise to fusion. Moreover, only under certain kinetic conditions will the enzyme give rise to the organization of non-lamellar structures that are conducive to the fusion event.     

High-power top-hat pulses from a Yb master oscillator power amplifier for efficient optical parametric amplifier pumping

We demonstrate shaping of high-energy broadband Yb amplifier pulses for the generation of a (sub)picosecond top-hat temporal pulse profile that significantly improves pumping efficiency of an optical parametric amplifier (OPA). Phase-only modulation is applied by an acousto-optic programmable dispersion filter. This simple scheme is scalable to a high average power due to a relatively broad bandwidth of the Yb:CaF(2) gain medium used in the amplifier that supports a sub-150-fs transform-limited pulse duration. Additionally we show that OPA seeding with supercontinuum remains possible because top-hat-shaped pulses passed through a glass block recompress to ≈200 fs with minimum satellite production.     

J/ψ polarization in pp collisions at √s=7 TeV

The ALICE Collaboration has studied J/ψ production in pp collisions at √s=7 TeV at the LHC through its muon pair decay. The polar and azimuthal angle distributions of the decay muons were measured, and results on the J/ψ polarization parameters λ(θ) and λ(φ) were obtained. The study was performed in the kinematic region 2.5相似文献   

Long-range correlations in the nonequilibrium quantum relaxation of a spin chain

We consider the nonstationary quantum relaxation of the Ising spin chain in a transverse field of strength h. Starting from a homogeneously magnetized initial state the system approaches a stationary state by a process possessing quasi-long-range correlations in time and space, independent of the value of h. In particular, the system exhibits aging (or lack of time-translational invariance on intermediate time scales) although no indications of coarsening are present.