Design and Synthesis of a Novel PLK1 Inhibitor Scaffold Using a Hybridized 3D-QSAR Model

Polo-like kinase 1 (PLK1) plays an important role in cell cycle progression and proliferation in cancer cells. PLK1 also contributes to anticancer drug resistance and is a valuable target in anticancer therapeutics. To identify additional effective PLK1 inhibitors, we performed QSAR studies of two series of known PLK1 inhibitors and proposed a new structure based on a hybridized 3D-QSAR model. Given the hybridized 3D-QSAR models, we designed and synthesized 4-benzyloxy-1-(2-arylaminopyridin-4-yl)-1H-pyrazole-3-carboxamides, and we inspected its inhibitory activities to identify novel PLK1 inhibitors with decent potency and selectivity.     

AMPS/AM/AMC14S三元共聚物的合成及应用

用引发聚合方法合成了AMPS／AM／AMC14S三元共聚物。对合成条件(AMPS／AM用量、反应温度、反应时间、单体纯度、单体浓度及除氧情况)进行了综合研究。研究表明,在单体总浓度10％～15％(ω)、引发剂浓度0．01％～0．02％(ω)、pH值为6时,在40℃反应8h以上可以得到转化率大于97％、特性粘数12dl／g的三元共聚物。性能评价表明,AMPS／AM／AMC14S三元共聚物耐温抗盐性较好。用AMPS／AM／AMC14S三元共聚物进行了弱凝胶调驱现场试验,取得了一定的增油降水的效果。     

Analysis of multispectral fields of satellite IR measurements: Using statistics of second spatial differential of spectral fields for measurement characterization

An approach using spatial analysis of satellite IR spectral measurements for quality assessment is presented. The second spatial differential is used as a model of measurement noise for spatially smooth radiative fields. Spatial differentiation significantly magnifies the noise contribution and reduces the physical signal amplitude because of differences in spatial distributions of instrument noise and atmospheric thermal fields. The second spatial differential represents a convenient and effective tool for numerical analysis of satellite IR measurements. This paper demonstrates that statistics of the second spatial differential are informative predictors for data‐quality characterization. Statistics of the second spatial differential are used for identifying anomalies in spectral channel data caused by detector noise, sensitivity loss to spatial shortwave thermal variations, and spatially (temporally) correlated noise.     

The smart city and its publics: insights from across six UK cities

In response to policy-makers’ increasing claims to prioritise ‘people’ in smart city development, we explore the publicness of emerging practices across six UK cities: Bristol, Glasgow, London, Manchester, Milton Keynes, and Peterborough. Local smart city programmes are analysed as techno-public assemblages invoking variegated modalities of publicness. Our findings challenge the dystopian speculative critiques of the smart city, while nevertheless indicating the dominance of ‘entrepreneurial’ and ‘service user’ modes of the public. We highlight the risk of bifurcation within smart city assemblages, such that the ‘civic’ and ‘political’ roles of the public become siloed into less obdurate strands of programmatic activity.     

LONG-TERM PERFORMANCE OF HOLLOW FIBRE MEMBRANE SOLVENT EXTRACTION MODULES USED FOR Cr(VI) RECOVERY FROM ELECTROPLATING RINSE WATER

ABSTRACT

The long-term performance of a hollow fibre membrane solvent extraction unit has been investigated for the recovery of Cr(VI) from plating rinse water. A pilot scale experiment was performed in a local electro-plating plant using-membrane modules with an area of 0·17 m². The separation of Cr(VI) from the rinse liquor was carried out in two hollow fibre membrane modules, and is compared with a single module supported liquid membrane (SLM) which was also used in the same service. The Cr(VI) flux declined gradually to half the initial value after 25 days. This was found to be due to the membrane fouling combined with the degradation of organic solvent. The loss of organic solution was initially severe but stabilized after a few days and became negligible. The flux in the SLM mode appeared similar but the life time was very short, less than a day, however continuous operation was attainable by periodic replenishment of the membrane. Using both designs, it has been shown that Cr(VI) could be extracted from dilute feed into the stripping solution with an enrichment factor of 10 – 20 times using this technique.     

Phenolic profile of blackberry wine produced using Korean winemaking techniques in earthenware jars

This research evaluated the winemaking potential of ‘Natchez’ and ‘Triple Crown’ blackberries grown in Oklahoma and examined the phenolic composition of blackberry wines made using modified Korean traditional winemaking techniques. The winemaking variables were fermentation temperature (21.6 vs 26.6°C), and fermentation type (yeast inoculation vs wild fermentation). High‐performance liquid chromatography was used to examine the phenolic compounds in blackberry juice and wine. The phenolic compounds consisted of anthocyanins (kuromanin, keracyanidin, delphinidin) and phenolic acids (gallic acid, catechin, caffeic acid, epicatechin, p‐coumaric acid). The ‘Natchez’ berries had higher concentrations of anthocyanins (kuromanin) while ‘Triple Crown’ berries had higher levels of phenolic acids (p‐coumaric acid). For many compounds, a higher fermentation temperature generally corresponded to higher concentrations of the phenolic compound in the wine after three months aging, but this was not universally observed. Accordingly, fermentation temperature may best be matched with individual cultivars via experimentation in order to maximise extraction and retention of phenolic compounds in the finished wines. Overall, the Korean traditional winemaking technique may be a good technique to add value to wines made from blackberries suited for production in a mid‐continental climate such as the central USA. © 2018 The Institute of Brewing & Distilling     

Design of a multichannel, multiresolution smart imaging system

This paper presents the design of a multichannel imaging system where the different optical channels have a different angular resolution and field-of-view. Such an imaging system is able to resolve fine details in a small region of interest through the channel that has the highest angular resolution (0.0096°) while controlling the surrounding region through the channel that has the widest field-of-view (2×40°). An interesting feature of such a multichannel, multiresolution imaging system is that various image processing algorithms can be applied at different segments of the image sensor. We have designed a three channel imaging system where each optical channel consists of four aspheric lens surfaces. These three imaging channels share a single image sensor with a resolution of 1440×960 and a 10 μm pixel size. All imaging channels have diffraction-limited performance ensuring good overall image quality.     

Effect of side groups in polynorbornene films for transparent conductive substrates

The imide-functionalized polynorbornene films exhibited excellent optical transparency in the visible range as well as high thermal stability over 200 degrees C. The indium tin oxide (ITO) thin films were coated on the imide-functionalized polynorbornene films at various deposition temperatures by employing radio-frequency (r.f.) planar magnetron sputtering system. The resulting ITO-coated imide-functionalized polynorbornene substrates showed good electrical and optical properties, while the figure of merit examination revealed that the present substrates are comparable to conventional ITO-glass substrates. This was confirmed from the preliminary result of organic light-emitting devices fabricated using the imide-functionalized polynorbornene substrates.     

Mathematical aspects of the meteorological interpretation of satellite hyperspectral infrared measurements part I: statement of the inverse problem for estimation of the cloud absorption vertical profile

Satellite high spectral resolution infrared measurements provide information for cloud vertical characterization when optically semi-transparent clouds at high altitude cover cloud layers at lower altitudes. It is an important issue because such atmospheric conditions are common and clouds are characterized by large-scale vertical development. An approximation radiative transfer model for a cloudy atmosphere is introduced. Cloud particle absorption of infrared (IR) radiation depends on the spectral frequency. So, the effective cloud parameters such as amount (absorption) and height, derived from IR spectral measurements, will be spectral functions as well. The degree of uncertainty in the determination of effective cloud parameters cannot be eliminated by increasing the number of spectral measurements. A cloud model should have extra degrees of freedom to address the spectral and spatial (vertical) variability of cloud absorption. A semi-discrete multilevel cloud model is used to describe the perturbation of the outgoing IR thermal radiation caused by cloudiness in the field of view of a satellite instrument. The model delineates cloudiness in a number of layers at fixed heights. Each layer (level) is characterized by the effective cloud absorption. An inverse problem of cloud absorption vertical profile (CAVP) estimation is described. The estimate of an effective cloud absorption profile is considered as predictor for identification of cloud presence at specific atmospheric layers. The problem is numerically examined for real satellite IR spectral measurements and solution estimates are compared with lidar measurements. Results show that the resulting estimate of CAVPs provides a realistic characterization of cloud top and cloud vertical scale.