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 .     

Finite Element Solution of Conical Diffraction Problems

This paper is devoted to the numerical study of diffraction by periodic structures of plane waves under oblique incidence. For this situation Maxwell's equations can be reduced to a system of two Helmholtz equations in R ² coupled via quasiperiodic transmission conditions on the piecewise smooth interfaces between different materials. The numerical analysis is based on a strongly elliptic variational formulation of the differential problem in a bounded periodic cell involving nonlocal boundary operators. We obtain existence and uniqueness results for discrete solutions and provide the corresponding error analysis.     

Compactness in fuzzy convergence spaces

Lowen and Lowen [Applications of category theory to fuzzy subsets (Kluwer, 1992) p. 153] and Lowen et al. [Fuzzy Sets and Systems 40 (1991) 347] recently introduced the category FCS of fuzzy convergence spaces, a topological quasitopos which is a supercategory of FTS, the category of fuzzy topological spaces. In this paper, compactness in FCS is examined. Doing so we found that to define compactness as an absolute property we had to generalize the definition of fuzzy convergence space to fuzzy subsets. All basic theorems are proved including the Tychonoff product theorem. Based on the theory developed here, in a following publication, a Richardson compactification for fuzzy convergence spaces will be given.     

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.