Synthesis and In Vivo antitumor and antiviral activities of 2′-deoxyribofuranosyl and arabinofuranosyl nucleosides of certain purine-6-sulfenamides,sulfinamides and sulfonamides

2′-Deoxyribofuranosyl and arabinofuranosyl nucleosides of certain purine-6-sulfenamides, sulfinamides and sulfonamides have been prepared by sequential amination and controlled oxidation of the corresponding 6-thiopurine nucleosides, and evaluated for antiviral and antitumor activities in mice. Amination of 2′-deoxy-6-thioinosine ( 4a ) and 9-β-D-arabinofuranosyl-6-thiopurine ( 4c ) with chloramine solution gave the corresponding 6-sulfenamides 5a and 5c , respectively, which on selective oxidation with 3-chloroperoxybenzoic acid (MCPBA) gave diastereomeric 9-(2-deoxy-β-D-erythro-pentofuranosyl)purine-6-sulfinamide ( 6a ) and 9-β-D-arabinofuranosylpurine-6-sulfinamide ( 6c ), respectively. However, oxidation of 5a and 5c with excess of MCPBA gave the corresponding 6-sulfonamide derivatives 7a and 7c , respectively. Similar amination of 2′-deoxy-6-thioguanosine ( 4b ), ara-6-thioguanine ( 4d ) and α-2′-deoxy-6-thioguanosine ( 8 ) gave the respective 6-sulfenamide derivatives 5b, 5d and 9 . Controlled oxidation of 5b, 5d and 9 gave (R,S)-2-amino-9-(2-deoxy-β-D-erythro-pentofuranosyl)purine-6-sulfinamide ( 6b ), (R,S)-2-amino-9-β-D-arabinofuranosylpurine-6-sulfinamide ( 6d ) and the α-anomer of ( 6b) (10 ), respectively. The diastereomeric mixture of (R,S )-10 was partially resolved and the structure of S -10 was assigned by single-crystal X-ray diffraction analysis. Oxidation of 5b, 5d and 9 with excess of MCPBA afforded the respective 6-sulfonamide derivatives 7b, 7d and 11 . Nucleosides 5c and 7c were significantly active against Friend leukemia virus in mice, whereas 6c was somewhat less active. Of the 20 nucleosides evaluated, 12 exhibited biologically significant anti-L1210 activity in mice. Nucleosides 6b and 7a at 173 mg/kg/day × 1 showed a T/C of 153, whereas 7d at 800 mg/kg/day × 1 showed a T/C of 153 against L1210 leukemia. The α-nucleoside 9 at 480 mg/kg/day × 1 gave a T/C of 172. A single treatment with 6b, 7a, 7d and 9 reduced the body burdens of viable L1210 cells by more than 99.2%. The antileukemic activity of these novel nucleosides tended to parallel solubility.     

子半理想环

本文提出了环论中的一个新概念：子半理想，得到了群环为子半理想环的一个充要条件。     

Lubrication of a rotating circular thrust bearing with a casson lubricant

Lubricants today are subjected to increasing mechanical shearing forces. This has resulted in an increasing interest in materials having variable viscosity. The problem of rotating circular thrust bearing is investigated with Casson fluid as a shear thinning lubricant. The pressure and load capacity of the thrust bearing is calculated when the feeding is done from the centre of the plates to the periphery. Also, moment of friction acting on the plates is calculated for different values of Casson number and for various values of ratio of inside to outside radius. It has been found that there is a decrease in the value of load capacity of the Casson lubricant. Also, it has been observed that there is an appreciable increase in the values of moment of friction for Casson fluid.     

传热传质对有抽吸的收缩薄片上的非线性磁流体动力学边界层流动的影响

This work is concerned with Magnetohydrodynamic viscous flow due to a shrinking sheet in the presence of suction. The cases of two dimensional and axisymmetric shrinking are discussed. The governing boundary layer equations are written into a dimensionless form by similarity transformations. The transformed coupled nonlinear ordinary differential equations are numerically solved by using an advanced numeric technique. Favorability comparisons with previously published work are presented. Numerical results for the dimensionless velocity, temperature and concentration profiles as well as for the skin friction, heat and mass transfer and deposition rate are obtained and displayed graphically for pertinent parameters to show interesting aspects of the solution.     

Scaling group transformation for the effect of temperature-dependent nanofluid viscosity on an mhd boundary layer past a porous stretching surface

This paper deals with a steady two-dimensional flow of an electrically conducting incompressible fluid over a porous vertical stretching sheet. The flow is permeated by a uniform transverse magnetic field. The fluid viscosity is assumed to vary as a linear function of temperature. The partial differential equations governing the problem under consideration are transformed by a special form of Lie group transformations, namely, scaling group of transformations, into a system of ordinary differential equations, which are solved numerically using the Runge-Kutta-Gill algorithm and the shooting method. The conclusion is drawn that the flow field and temperature profiles are significantly influenced by the Lewis number, Brownian motion number, and thermophoresis number.     

Structure and conformation of a nickel complex: {2‐Hydroxo‐3‐piperidine‐1‐yl‐methyl‐N,N′(bis‐5‐bromobenzylpropylenediimine)nickel(II)perchlorate}

The title compound, a nickel complex [C₂₃H₂₆N₃O₂Br₂Ni.(ClO₄)] (CCDC 199520) crystallizes in triclinic space group P with the cell parameters a = 10.2560(4), b = 10.8231(4), c = 12.0888(5)Å, α = 99.404(1), β = 99.780(1), γ = 92.252(1)° and V = 1301.49(9)ų. The structure was solved by Patterson method and refined by full‐matrix least‐squares procedures to a final R = 0.0497 using 6287 observed reflections. In the complex, the piperidine ring takes chair conformation and the geometry around the Ni ion is slightly distorted square planar. The dihedral angle between the planes [N‐Ni‐N and O‐Ni‐O] is 9.4(1)°. The chelate ring containing both the nitrogen atoms adopts twisted boat conformation. The molecules in the crystal are stabilized by N‐H…O and C‐H…O types of hydrogen bonds in addition to a C‐H…π interaction. (© 2004 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim)