Synthesis and comparative molecular field analysis (CoMFA) of antitumor 3-arylisoquinoline derivatives

In this study a series of 3-arylisoquinoline derivatives were synthesized and cytotoxicity against human melanoma tumor cell evaluated, and a three dimensional quantitative structure-activity relationship was investigated using the comparative molecular field analysis (CoMFA). The results suggested that the electrostatic, steric and hydrophobic factors of 3-arylisoquinolines were strongly correlated with the antitumor activity. Considerable predictive ability (cross-validated r2 as high as 0.721) was obtained through CoMFA.     

An optimal instruction scheduler for superscalar processor

Performance in superscalar processing strongly depends on the compiler's ability to generate codes that can be executed by hardware in an optimal or near optimal order. Generating optimal code is an NP-complete problem. However, there is a need for highly optimized code, such as in superscalar or real-time systems. In this paper, an instruction scheduling scheme for optimizing a program trace is proposed. Optimized code can be arrived at without much redundant work, if some important features in code are well explored and utilized in scheduling. To formalize the task, two abstract models, one for a superscalar processor and the other for a program trace, are given. These two models reflect most of the characteristics of the scheduling problem. The interrelations between instructions and partial schedules are thoroughly studied, and dominance and equivalence relations on them are defined. These relations are then used to reduce the solution space and eventually help to produce optimal schedules. The results of experiments that show the promise of the proposed scheme are also presented     

Characterization of arylamine N-acetyltransferase in Enterobacter aerogenes

N-acetyltransferase (NAT) activity was determined by incubation of purified Enterobacter aerogenes enzyme with 2-aminofluorene (2-AF) as the substrate, followed by high pressure liquid chromatography assays. The NAT activity from E. aerogenes was 0.58 +/- 0.08 nmol/min/mg protein for 2-AF. The values of apparent K(m) and Vmax were 0.72 +/- 0.14 mM and 2.45 +/- 0.29 nmol/min/mg protein, respectively, for 2-AF. The optimal pH value for the enzyme activity was 7.5 for the 2-AF tested. The optimal temperature for enzyme activity was 37 degrees C for the 2-AF substrate. The molecular weight of NAT from E. aerogenes was 44.9 kD. Among a series of divalent cations and salts, Zn2+, Ca2+, and Fe2+ were demonstrated to be the most potent protease inhibitors, and only ethylenediaminetetraacetic acid significantly protected the NAT. Iodoacetamide, in contrast to other agents, markedly inhibited NAT.     

Intelligent copyright protection system using a matching video retrieval algorithm

Many video service sites headed by YouTube know what content requires copyright protection. However, they lack a copyright protection system that automatically distinguishes whether uploaded videos contain legal or illegal content. Existing protection techniques use content-based retrieval methods that compare the features of video. However, if the video encoding has changed in resolution, bit-rate or codec, these techniques do not perform well. Thus, this paper proposes a novel video matching algorithm even if the type of encoding has changed. We also suggest an intelligent copyright protection system using the proposed algorithm. This can serve to automatically prevent the uploading of illegal content. The proposed method has represented the accuracy of 97% with searching algorithm in video-matching experiments and 98.62% with automation algorithm in copyright-protection experiments. Therefore, this system could form a core technology that identifies illegal content and automatically excludes access to illegal content by many video service sites.     

Predictive simulation of human walking transitions using an optimization formulation

A general optimization formulation for transition walking prediction using 3D skeletal model is presented. The formulation is based on a previously presented one-step walking formulation (Xiang et al., Int J Numer Methods Eng 79:667–695, 2009b). Two basic transitions are studied: walk-to-stand and slow-to-fast walk. The slow-to-fast transition is used to connect slow walk to fast walk by using a step-to-step transition formulation. In addition, the speed effects on the walk-to-stand motion are investigated. The joint torques and ground reaction forces (GRF) are recovered and analyzed from the simulation. For slow-to-fast walk transition, the predicted ground reaction forces in step transition is even larger than that of the fast walk. The model shows good correlation with the experimental data for the lower extremities except for the standing ankle profile. The optimal solution of transition simulation is obtained in a few minutes by using predictive dynamics method.     

Effect of stress-strain-law transients on formability

The effect of work-hardening changes, of the type that follow a rapid change of strain state or strain rate, on formability has been investigated using finite element modeling (FEM). A standard sheet tensile test was chosen as an arbitrary forming operation and a rigid-viscoplastic FEM program was employed for analysis. In each case, a transitional region of true strains between 0.1 and 0.2 was modeled. Transients involving lowered work-hardening rates (negative value of An) promoted increased strain localization and premature failure while transients with increased work-hardening rates enhanced formability. Total engineering elongations (50 mm gage length) varied between 20 pct and 46 pct, illustrating the importance of the transient far beyond the transient region. The controlling factor is the effective work-hardening rate in the transient region rather than the change in strength coefficient or flow stressper se. A direct stress offset of the flow curve { } also affects strain localization through a change in effective work-hardening rate.     

A Chinese information processing system

The Chinese information processing system(CIPS)introduced in this paper can producegraphs,tables,flowcharts,mathematical equations,forms and also provides typesettingfacilities.The system can process not only Chinese text but also English text or a mixture ofthem.It is written in C language and runs on VAX Ⅱ/780 under Unix operating system.TheCIPS system is very easy to use and provides user-defined macro which allows abbreviationsof commonly used Chinese phrases and reduce the complexity of Chinese characters coding.     

A study on the dynamic characteristics of the Korean Yi-dynasty bell type structure

The dynamic characteristics of the Korean Yi-dynasty bell type structure, including the acoustic effects, are analyzed both theoretically and experimentally. The numerical solutions of natural frequencies and mode shape for membrane and flexural behavior are obtained by using the NASTRAN program for the finite element method with plate shell elements of triangular and quadrilateral types. Test bells, A and B types similar to the Kap-Sa bell in Kong-Ju chosen among typical Korean Yi-dynasty bells, are manufactured on different scales to the original bell. To consider the effects of the variation of the structural dimension on the dynamic response, these bells are analyzed with respect to the variation of the thickness of the wall and the bottom rim and the asymmetric Dang-Jwas. The impact method with the Fast Fourier Transform Analyzer is adopted to experimentally assess the dynamic response. Results are in good agreement with the numerical solutions.     

Molecular Docking Studies and Biological Evaluation of Berberine–Benzothiazole Derivatives as an Anti-Influenza Agent via Blocking of Neuraminidase

In this study, we have introduced newly synthesized substituted benzothiazole based berberine derivatives that have been analyzed for their in vitro and in silico biological properties. The activity towards various kinds of influenza virus strains by employing the cytopathic effect (CPE) and sulforhodamine B (SRB) assay. Several berberine–benzothiazole derivatives (BBDs), such as BBD1, BBD3, BBD4, BBD5, BBD7, and BBD11, demonstrated interesting anti-influenza virus activity on influenza A viruses (A/PR/8/34, A/Vic/3/75) and influenza B viral (B/Lee/40, and B/Maryland/1/59) strain, respectively. Furthermore, by testing neuraminidase activity (NA) with the neuraminidase assay kit, it was identified that BBD7 has potent neuraminidase activity. The molecular docking analysis further suggests that the BBD1–BBD14 compounds’ antiviral activity may be because of interaction with residues of NA, and the same as in oseltamivir.