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 .     

Shell model interaction between proton holes and between proton holes and neutron particles around 208Pb

An effective residual interaction between particles and holes for shell model calculations around ²⁰⁸Pb, derived from the interaction between free nucleons, is compared with the measured properties of proton-hole neutron states in ²⁰⁸Tl and the interaction between proton holes is adjusted to newly measured level energies in ²⁰⁶Hg. These interaction elements are particularly relevant for neutron-rich nuclei. The adjustment of two mixing elements reproduces the known γ-decay data in ²⁰⁸Tl. Received: 2 April 2002 / Accepted: 2 May 2002     

Effective Mode Volume of Nanoscale Plasmon Cavities

The controlled squeezing of electromagnetic energy into nanometric volumes via surface plasmon-polariton excitations in plasmonic nanoresonators is analyzed using the concept of an effective electromagnetic mode volume V _eff, while taking careful account of the plasmon-polariton dispersion and the electromagnetic energy stored in the metal. Together with the quality factor Q of the cavity resonance, this enables a comparison with dielectric optical cavities, where V _eff is limited by diffraction. For a Fabry–Perot type planar metallic cavity, a one-dimensional analytic model as well as a three-dimensional finite-difference time-domain simulation reveal that V _eff is not bounded by diffraction, and that Q/V _eff increases for decreasing cavity size. In this picture, matter–plasmon interactions can be quantified in terms of Q and V _eff, and a resonant cavity model for the enhancement of spontaneous Raman scattering is presented.