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.     

Study of the reaction238U (α, α′f) atE α=480 MeV

The excitation function of the fission probability P _E E _x) for²³⁸U has been measured in the reaction²³⁸U(α, α′ f) at 480 MeV bombarding energy. The reaction mechanism of this reaction is discussed for excitation energies belowB _nf , the threshold for second chance fission, and aboveB _nf up toE _x =37 MeV. In comparing with results from fission induced by photons and by particle transfer reactions the (α, α′f) reaction gives too low values for the fission probabilityP _f at excitation energies well aboveB _nE . The role of the quasi-elastic knock-out process in this reaction is discussed.     

Ground-state properties of LiV2O4 and Li1-xZnx(V1-yTiy)2O4

We present susceptibility, microwave resistivity, NMR and heat-capacity results for Li_1-xZn_x(V_1-yTi_y)₂O₄ with 0 ? x ? 0.3 and 0 ? y ? 0.3. For all doping levels the susceptibility curves can be fitted with a Curie-Weiss law. The paramagnetic Curie-Weiss temperatures remain negative with an average value close to that of the pure compound Θ≈ - 36 K. Spin-glass anomalies are observed in the susceptibility, heat-capacity and NMR measurements for both type of dopants. From the temperature dependence of the spin-lattice relaxation rate we found critical-dynamic behavior in the Zn doped compounds at the freezing temperatures. For the Ti-doped samples two successive freezing transitions into disordered low-temperature states can be detected. The temperature dependence of the heat capacity for Zn-doped compounds does not resemble that of canonical spin glasses and only a small fraction of the total vanadium entropy is frozen at the spin-glass transitions. For pure LiV₂O₄ the spin-glass transition is completely suppressed. The temperature dependence of the heat capacity for LiV₂O₄ can be described using a nuclear Schottky contribution and the non-Fermi liquid model, appropriate for a system close to a spin-glass quantum critical point. Finally an ( x / y , T )-phase diagram for the low-doping regime is presented. Received 16 March 2001 and Received in final form 30 October 2001     

Structure of neutron-rich Be and C isotopes

The structure of neutron-rich beryllium isotopes has been investigated using different heavy-ion-induced transfer reactions. In neutron transfer reactions, the population of final states shows a strong sensitivity to the chosen core nucleus, i.e., the target nuclei ⁹Be or ¹⁰Be, respectively. Molecular rotational bands up to high excitation energies are observed with ⁹Be as the core due to its pronounced 2α-cluster structure, whereas only a few states at low excitation energies are populated with ¹⁰Be as the core. For ¹¹Be, a detailed investigation has been performed for the three states at 3.41, 3.89, and 3.96 MeV, which resulted in the most probable spin-parity assignments 3/2⁺, 5/2^?, and 3/2^?, respectively. Furthermore, we have studied particle-hole states of ¹⁶C using the ¹³C(¹²C, ⁹C)¹⁶C reaction and found 14 previously unknown states. Using the ¹²C(¹²C, ⁹C)¹⁵C reaction, five new states were observed for ¹⁵C.     

Über die Einwirkung von Ammoniak auf Anthragallol

Ohne ZusammenfassungDiese Untersuchung ist vor mehr als Jahresfrist infolge Eintrittes in die chemische Praxis abgebrochen worden. Äussere Verhältnisse machen die Vollendung der begonnenen Versuche auch weiterhin unmöglich und sehe ich mich desshalb veranlasst, meine Beobachtungen zu veröffentlichen.