DNA-Directed alkylating agents. 7. Synthesis, DNA interaction, and antitumor activity of bis(hydroxymethyl)- and bis(carbamate)-substituted pyrrolizines and imidazoles

A series of bis(hydroxymethyl)-substituted imidazoles, thioimidazoles, and pyrrolizines and related bis(carbamates), linked to either 9-anilinoacridine (intercalating) or 4-(4-quinolinylamino)benzamide (minor groove binding) carriers, were synthesized and evaluated for sequence-specific DNA alkylation and cytotoxicity. The imidazole and thioimidazole analogues were prepared by initial synthesis of [(4-aminophenyl)alkyl]imidazole-, thioimidazole-, or pyrrolizine dicarboxylates, coupling of these with the desired carrier, and reduction to give the required bis(hydroxymethyl) alkylating moiety. The pyrrolizines were the most reactive alkylators, followed by the thioimidazoles, while the imidazoles were unreactive. The pyrrolizines and some of the thioimidazoles cross-linked DNA, as measured by agarose gel electrophoresis. Strand cleavage assays showed that none of the compounds reacted at purine N7 or N3 sites in the gpt region of the plasmid gpt2Eco, but the polymerase stop assay showed patterns of G-alkylation in C-rich regions. The corresponding thioimidazole bis(carbamates) were more selective than the bis(hydroxymethyl) pyrrolizines, with high-intensity bands at 5'-NCCN, 5'-NGCN and 5'-NCGN sequences in the PCR stopping assay ( indicates block sites). The data suggest that these targeted compounds, like the known thioimidazole bis(carbamate) carmethizole, alkylate exclusively at guanine residues via the 2-amino group, with little or no alkylation at N3 and N7 guanine or adenine sites. The cytotoxicities of the compounds correlated broadly with their reactivities, with the bis(hydroxymethyl)imidazoles being the least cytotoxic (IC50s >1 microM; P388 leukemia) and with the intercalator-linked analogues being more cytotoxic than the corresponding minor-groove-targeted ones. This was true also for the more reactive thioimidazole bis(carbamates) (IC50s 0.8 and 11 microM, respectively), but both were more active than the analogous "untargeted" carmethizole (IC50 20 microM). The bis(hydroxymethyl)pyrrolizine analogues were the most cytotoxic, with IC50s as low as 0.03 microM.     

图的正交(g,f)-因子分解

设ｇ和ｆ分别是定义在图Ｇ的顶点集合Ｖ（Ｇ）上的整数值函数且对每一个ｘ∈Ｖ（Ｇ）有２≤ｇ（ｘ）≤ｆ（ｘ）．证明了若Ｇ是（ｍｇ＋ｍ－１,ｍｆ－ｍ＋１）—图,则对Ｇ中任意一个给定的有ｍ条边的子图Ｈ,Ｇ有一个（ｇ,ｆ）—因子分解与Ｈ正交．     

Sentiment-oriented contextual advertising

Web advertising (Online advertising), a form of advertising that uses the World Wide Web to attract customers, has become one of the world’s most important marketing channels. This paper addresses the mechanism of Content-based advertising (Contextual advertising), which refers to the assignment of relevant ads to a generic web page, e.g., a blog post. As blogs become a platform for expressing personal opinion, they naturally contain various kinds of expressions, including both facts and comments of both a positive and negative nature. Besides, in line with the major tenet of Web 2.0 (i.e., user-centric), we believe that the web-site owners would be willing to be in charge of the ads which are positively related to their contents. Hence, in this paper, we propose the utilization of sentiment detection to improve Web-based contextual advertising. The proposed sentiment-oriented contextual advertising (SOCA) framework aims to combine contextual advertising matching with sentiment analysis to select ads that are related to the positive (and neutral) aspects of a blog and rank them according to their relevance. We experimentally validate our approach using a set of data that includes both real ads and actual blog pages. The results indicate that our proposed method can effectively identify those ads that are positively correlated with the given blog pages.     

Dynamically modulated intensity interrogation scheme using waveguide coupled surface plasmon resonance sensors

An electro-optically modulated intensity interrogation method based on tunable waveguide coupled surface plasmon resonance sensors has been proposed. It has been theoretically and experimentally demonstrated that the proposed scheme can enable sensitive measurement of measurand variations. By modulating the refractive index in the waveguide layer, this interrogation method yields modulated signal whose amplitude is related to measurand's refractive index. This amplitude modulated signal offers a higher signal to noise ratio and eliminates additive noise in the sensor system. A preliminary investigation using saline buffers with different NaCl concentrations shows a resolution of 2.3 × 10^?6 refractive index unit by our approach. Resolution can be controlled by the amplitude of the applied modulation voltage and can be further enhanced by optimizing the device structure or improving the electro-optical (E-O) coefficient of the E-O material. This approach is simple, stable, and promising for low-cost or multi-channel SPR biosensor applications.     

变频器故障分析及处理

从参数设置、过电压、过电流、过负载等方面详细分析了变频器常见故障产生的原因及处理方法.     

A divide-and-conquer hole-filling method for handling disocclusion in single-view rendering

Large holes are unavoidably generated in depth image based rendering (DIBR) using a single color image and its associated depth map. Such holes are mainly caused by disocclusion, which occurs around the sharp depth discontinuities in the depth map. We propose a divide-and-conquer hole-filling method which refines the background depth pixels around the sharp depth discontinuities to address the disocclusion problem. Firstly, the disocclusion region is detected according to the degree of depth discontinuity, and the target area is marked as a binary mask. Then, the depth pixels located in the target area are modified by a linear interpolation process, whose pixel values decrease from the foreground depth value to the background depth value. Finally, in order to remove the isolated depth pixels, median filtering is adopted to refine the depth map. In these ways, disocclusion regions in the synthesized view are divided into several small holes after DIBR, and are easily filled by image inpainting. Experimental results demonstrate that the proposed method can effectively improve the quality of the synthesized view subjectively and objectively.     

设计管理系统信息需求的分析与实现

对信息需求的准确分析是建立设计管理系统的基础。传统的分析方法从过程与人,过程与信息的角度出发综合分析整个机构的信息需求,但是,这种方法没有示识产生和使用信息的范围。为此,;补充分析了信息的机构和项目属性,并通过建立三维组织机构模型;机械、人员和任务模型,有效控制基本的信息存取。     

自然主义——新艺术者的梦幻出口——浅析自然主义在设计史上盛极而衰的原因

自然主义对许多艺术门类都产生过深刻影响,在设计领域中,以自然主义为主要特点的新艺术运动曾在一个重大的设计变革时期——工业革命后风靡各国,然而却又在短短十多年后沉寂下来,本文主要分析自然主义为什么会在设计史的重要阶段产生如此特别的表现。