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.     

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 .     

Dynamic interaction of plasma flow with the hot boundary layer of a geomagnetic trap

The study of the interaction between collisionless plasma flow and stagnant plasma revealed the presence of an outer boundary layer at the border of a geomagnetic trap, where the super-Alfvén subsonic laminar flow changes over to the dynamic regime characterized by the formation of accelerated magnetosonic jets and decelerated Alfvén flows with characteristic relaxation times of 10–20 min. The nonlinear interaction of fluctuations in the initial flow with the waves reflected from an obstacle explains the observed flow chaotization. The Cherenkov resonance of the magnetosonic jet with the fluctuation beats between the boundary layer and the incoming flow is the possible mechanism of its formation. In the flow reference system, the incoming particles are accelerated by the electric fields at the border of boundary layer that arise self-consistently as a result of the preceding wave-particle interactions; the inertial drift of the incoming ions in a transverse electric field increasing toward the border explains quantitatively the observed ion acceleration. The magnetosonic jets may carry away downstream up to a half of the unperturbed flow momentum, and their dynamic pressure is an order of magnitude higher than the magnetic pressure at the obstacle border. The appearance of nonequilibrium jets and the boundary-layer fluctuations are synchronized by the magnetosonic oscillations of the incoming flow at frequencies of 1–2 mHz.     

The magnetization behavior of nanocrystalline permanent magnets based on the Stoner–Wohlfarth Model

The magnetization behavior in nanocrystalline permanent magnets has been investigated using mean field Stoner–Wohlfarth model. The model is comparatively simple but allows the numerical treatment of extended nanostructures. The predominant intergrain exchange coupling is expressed by a mean field constant N_m in spite of no explicit relationship between N_m and the microstructure. By this model, the experimental phenomena, such as the remanence enhancement, the shape of demagnetization curve, the irreversible magnetization, the exchange bias field and their respective temperature dependence, can be well explained. The N_m dependence of magnetic properties has been extensively discussed in the present paper.     

Level of nodes in increasing trees revisited

Simply generated families of trees are described by the equation T(z) = ϕ(T(z)) for their generating function. If a tree has n nodes, we say that it is increasing if each node has a label ∈ { 1,…,n}, no label occurs twice, and whenever we proceed from the root to a leaf, the labels are increasing. This leads to the concept of simple families of increasing trees. Three such families are especially important: recursive trees, heap ordered trees, and binary increasing trees. They belong to the subclass of very simple families of increasing trees, which can be characterized in 3 different ways. This paper contains results about these families as well as about polynomial families (the function ϕ(u) is just a polynomial). The random variable of interest is the level of the node (labelled) j, in random trees of size n ≥ j. For very simple families, this is independent of n, and the limiting distribution is Gaussian. For polynomial families, we can prove this as well for j,n → ∞ such that n − j is fixed. Additional results are also given. These results follow from the study of certain trivariate generating functions and Hwang's quasi power theorem. They unify and extend earlier results by Devroye, Mahmoud, and others. © 2007 Wiley Periodicals, Inc. Random Struct. Alg., 2007