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.     

Ueber die in der Milch enthaltenen Eiweissk?rper

Ohne Zusammenfassung     

Quaternions for GUTs

We derive an appropriate definition of transpose for quaternionic matrices and give a new panoramic review of the quaternionic groups. We aim to analyze possible quaternionic groups for GUTs.     

Giant shot-like voltage noise in high current density Nb–AlOx–Nb superconducting tunnel junctions

The flat voltage noise component of current biased, high-transparency Nb/AlO_x/Nb superconducting tunnel junctions has been investigated at frequencies up to 70 kHz. Several aspects of the analyzed phenomena suggest the presence of current noise effects induced by the discreteness of the charge carriers. At subgap voltages, where excess currents occur, a behavior coherent with a multiple Andreev reflection-assisted transport through the tunnel barrier has been found. However, the measured charge values exceed any theoretical prediction.     

Existence of solutions to projected differential equations in Hilbert spaces

We prove existence and uniqueness of integral curves to the (discontinuous) vector field that results when a Lipschitz continuous vector field on a Hilbert space of any dimension is projected on a non-empty, closed and convex subset.

     

The Loewner Equation: Maps and Shapes

An approach called Schramm–Loewner evolution (SLE) provides a new method for dealing with a wide variety of scale-invariant problems in two dimensions. This approach is based upon an older method called Loewner Evolution (LE), which connects analytic and geometrical constructions in the complex plane. In this paper, the bases of LE and SLE are described and some simple applications are discussed in relatively non-technical form. A bibliography of the subject is presented.     

A simple expression for the ADM mass

We show by an almost elementary calculation that the ADM mass of an asymptotically flat space can be computed as a limit involving a rate of change of area of a closed 2-surface. The result is essentially the same as that given by David Brown and York (Phys. Rev. D 55, 1977–1984 1997; Phys. Rev. D 47, 1407–1419 1993). We will prove this result in two ways, first by direct calculation from the original formula as given by Arnowitt, Deser and Misner and second as a corollary of an earlier result by Brewin for the case of simplicial spaces.