Nitrostyrene Derivatives of Adenosine 5′-Glutarates Modified with an Alkyl Spacer and their inhibitory activity on epidermal growth factor receptor protein tyrosine kinase

β-Nitrostyrene derivatives of adenosine 5′-glutarates are potent and selective bisubstrate-type inhibitors of the epidermal growth factor receptor protein tyrosine kinase (EGF-R PTK). In an attempt to improve the inhibitory activity, this type of compounds was modified with alkyl spacers of varying length between the nitrostyrene and the glutaryl units. The spacers consisted of 1, 3, 4, and 5 atoms to give compounds of the benzyl, oxyethyl, oxypropyl, and oxybutyl series, respectively (Schemes 1 and 2). Adenosine 5′-esters were prepared in the benzyl and oxypropyl series only. Compared to the compounds in the parent series without spacer (IC₅₀ = 0.7–12 μM ), most of the modified compounds inhibited the EGF-R PTK only marginally or were inactive (IC₅₀ ≥ 100 μM ). The only exceptions were the free acids 19 and 20 with IC₅₀ values of ca. 5 μM . It is noteworthy that esterification of these two hydrogen glutarates with either MeOH or adenosine yielded inactive compounds, which is in contrast to the corresponding substances without spacers.     

Derivatives of (2R)-N-Glyoxylbornane-10,2-sultam and Their Use as auxiliaries in the diastereoselective spirocyclization of 2-substituted tryptamines

A crude hydrate 6 and a crystalline hemiacetal 7 of glyoxylamide 4 were prepared from crotonamide 5 (Scheme 2). Particularly hemiacetal 7 , but also 6 and the ‘dimer’ 8 (obtained from 7 ) may serve as homochiral auxiliaries. The structure of 8 was determined by X-ray analysis. By arenesulfonyl halides, tryptimines 12–14 of 4 were diastereoselectively transformed into spirotricycles 15–17 and 19 .     

Synthesis of Benzazepine Analogues of Noscapine

The synthesis of benzazepine analogues of the opium alkaloid noscapine ( 1 ) is described. The benzazepines 2 and 3 were prepared starting from nornarceine ethyl ester ( 4 ; readily available from 1 ) in several steps. X-Ray analysis of compound 2 revealed that it is not a diastereosisomer mixture but a racemate of the threo-form and thus has the same configuration as 1 .     

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The helium atom in its ground state, subject to strong magnetic fields, is treated using a variational method. Trial functions consisting of Gaussians with nonlinear parameters variationally optimized are used. The form of these functions is a generalized s-symmetry-state properly modified to admit spatial deformation along the direction on which the magnetic field is applied. © 1994 John Wiley & Sons, Inc.     

Dynamic study of gated saturable absorbers

The capability of gated saturable absorbers for single-pulse selection is studied theoretically using the classical space-time-dependent rate-equation model. The dynamics of operation is followed experimentally by the well-known pump—probe technique. Comparing the theoretical and experimental results, it is found that gated saturable absorbers can efficiently be used for pulse forming and pulse selection of pulses longer than picosecond.     

The external magnetic field dependence of RF splitting of57Fe hyperfine lines. NMR + Mössbauer double resonance experiment

We present the results of an experimental investigation of a RF splitting of⁵⁷Fe hyperfine lines in the regime of NMR and Mössbauer double resonance. The experiments have been performed as a function of RF field intensity and static magnetic field magnitude. The intensity of the RF components and the separation between them are extremely sensitive to the frequency and amplitude of the RF magnetic field. The RF splitting of hyperfine lines is inversely proportional to the strength of the static magnetic field.     

Electrodialysis of Hydrosols of Ultradispersed Diamonds

The electrical conductivity of hydrosols of ultradispersed diamonds was studied. The electromembrane method for cleaning and concentrating of ultradispersed diamonds in hydrosols was considered. The influence exerted by the concentration of the dispersed phase on the electrical characteristics of the cleaning process was analyzed. A mathematical relation making it possible to evaluate the output characteristics of the process and to determine the geometrical characteristics of the apparatus was proposed.     

Radiation bursts from particles in the field of compact, impenetrable, astrophysical objects

The radiation emitted by charged, scalar particles in a Schwarzschild field with maximal acceleration corrections is calculated classically and in the tree approximation of quantum field theory. In both instances the particles emit radiation that has characteristics similar to those of gamma-ray bursters.