Hit to Leads with Cytotoxic Effect in Leukemic Cells: Total Synthesis Intermediates as a Molecule Treasure Chest

A previously designed and developed 12-step total synthesis that includes [1,1′-biphenyl]-2-amine and carbazole intermediates and that ultimately produces the carbazole alkaloid carbazomycin G was exploited as a screening compound library with the goal of identifying potential lead compound(s) with cytotoxic effect. These compounds were investigated by using in-vitro tests involving the two human cell lines HL-60 and MOLM-13, which both model acute myeloid leukaemia (AML). The in-vitro biological test results were used together with the molecular structures of the various intermediates in a concise SAR analysis. Several of the intermediates revealed cytotoxicity (IC₅₀<10⁻⁴ M), although the final natural product carbazomycin G did not reveal cytotoxicity versus the two said human cell lines.     

洼60-H26水平井套铣打捞技术

洼60-H26井是一口中曲率水平井,设计井深1 922 m,由于地面条件的限制,设计采用三维井眼轨道。该井水平段在钻至井深1 801 m时,发生卡钻事故。在卡钻事故处理过程中,采用测卡、爆炸松扣技术取出上部钻具后,应用了不同规格的套铣管对被卡钻具进行套铣,采用间歇式套铣方式实现了大斜度井段(45°-90°)的安全套铣,采用短套铣管完成了时水平井段内φ215．0 mm稳定器的套铣,采用φ228．6 mm套铣管成功套铣水平井段被卡LWD仪器,最后通过震击器震击成功解卡。详细介绍了洼60-H26水平井卡钻事故的处理过程,分析了在水平段处理卡钻事故的难点。该井处理卡钻事故的经验,对以后水平井施工中处理井下事故、打捞贵重仪器具有借鉴价值。     

Non-deterministic exponential time has two-prover interactive protocols

We determine the exact power of two-prover interactive proof systems introduced by Ben-Or, Goldwasser, Kilian, and Wigderson (1988). In this system, two all-powerful noncommunicating provers convince a randomizing polynomial time verifier in polynomial time that the inputx belongs to the languageL. We show that the class of languages having tow-prover interactive proof systems is nondeterministic exponential time.We also show that to prove membership in languages inEXP, the honest provers need the power ofEXP only.The first part of the proof of the main result extends recent techniques of polynomial extrapolation used in the single prover case by Lund, Fortnow, Karloff, Nisan, and Shamir.The second part is averification scheme for multilinearity of a function in several variables held by an oracle and can be viewed as an independent result onprogram verification. Its proof rests on combinatorial techniques employing a simple isoperimetric inequality for certain graphs:     

Semiparametric Estimation in Time‐Series Regression with Long‐Range Dependence

Abstract. We consider semiparametric estimation in time‐series regression in the presence of long‐range dependence in both the errors and the stochastic regressors. A central limit theorem is established for a class of semiparametric frequency domain‐weighted least squares estimates, which includes both narrow‐band ordinary least squares and narrow‐band generalized least squares as special cases. The estimates are semiparametric in the sense that focus is on the neighbourhood of the origin, and only periodogram ordinates in a degenerating band around the origin are used. This setting differs from earlier studies on time‐series regression with long‐range dependence, where a fully parametric approach has been employed. The generalized least squares estimate is infeasible when the degree of long‐range dependence is unknown and must be estimated in an initial step. In that case, we show that a feasible estimate which has the same asymptotic properties as the infeasible estimate, exists. By Monte Carlo simulation, we evaluate the finite‐sample performance of the generalized least squares estimate and the feasible estimate.     

C60辅助下ZnNiS光催化分解水制备氢气的研究

通过在光催化剂掺杂ZnS中加入球笼化合物富勒烯C60,提高了光催化水分解的效率.并采用气相色谱法跟踪反应,发现氢气释放量是未加C60时的4倍多.同时,对该催化反应的机理进行了初步的探讨.     

A new way for constructing high accuracy shock-capturing generalized compact difference schemes

The generalized compact (GC) schemes and some of their important properties are presented. And a new way for constructing high order accuracy and high-resolution GC schemes is presented. The schemes constructed by using this way could satisfy some principles and demands prescribed in advance to ensure some desired properties to the schemes, such as the principle about suppression of the oscillations, the principle of stability, the order of accuracy and number of scheme points, etc. As two examples, a three-point third-order compact scheme and a three-point fifth-order GC scheme satisfying the principle about suppression of the oscillations and the principle of stability are described in this paper. Numerical results show that these schemes are shock-capturing. The time-dependent boundary conditions proposed by Thompson are well employed when the algorithm is applied to the Euler equations of gas dynamics. Fourier analysis shows that the resolution characteristics are spectral-like.     

RADIATION FIELD FROM A RECTANGULAR PLAQUE SOURCE FOR RADIATION PROCESSING

Evaluation of the Hubbell integral for an omnidirectional detector response to a rectangular plaque gamma emitting radiation source using a different numerical computation method on a personal computer was made. For a plaque consisting of several strip gamma emitters, exposure rates at different positions above the source were calculated using 'exact' evaluation and an approximate method. Optimization method is used to find source activity of each strip, so as to acquire desirable dose uniformity of the irradiated products. In uses of the Hubbell integral, by introducing appropriate programming, computation time can be saved.     

Influence of Missing Values on the Prediction of a Stationary Time Series

Abstract. The influence of missing observations on the linear prediction of a stationary time series is investigated. Simple bounds for the prediction error variance and asymptotic behaviours for short and long‐memory processes respectively are presented.     

Kinetic Studies of the Thermal Decomposition of C60H2 in Solution

Thermal decomposition of C₆₀H₂ in C₆D₄Cl₂ solution at 236°C for 2 hours was shown to produce hydrogen as a product, the hydrogen production was successfully followed by NMR. In order to further explore the rule of thermal decomposition of C₆₀H₂, the dynamics of decomposition reaction was studied and the results showed this decomposition reaction accorded with first order reaction dynamical equation. The experiment temperature was ranged separately in 459K, 455K, 451K, and 446K.     

Two Isomers of C60F48: Computed Inter-isomeric Equilibrium

C₆₀F₄₈ has been known to exist in two isomeric forms of D₃ and S₆ symmetries. However, the quantum-chemical calculations have not agreed on their stability order though a near-isoenergetic picture is otherwise always encountered. In order to clarify the situation, the entropy effects are evaluated for synthetic temperatures of about 500K. The entropy evaluations suggest that the D₃ isomer should be more stable in the potential energy by 2.05-2.55 kcal/mol (to which term the ab initio data are closer than the semiempirical ones).