Apparate

Ohne Zusammenfassung     

C6-C8 bridged epothilones: consequences of installing a conformational lock at the edge of the macrocycle

A series of conformationally restrained epothilone analogues with a short bridge between the methyl groups at C6 and C8 was designed to mimic the binding pose assigned to our recently reported EpoA-microtubule binding model. A versatile synthetic route to these bridged epothilone analogues has been successfully devised and implemented. Biological evaluation of the compounds against A2780 human ovarian cancer and PC3 prostate cancer cell lines suggested that the introduction of a bridge between C6-C8 reduced potency by 25-1000 fold in comparison with natural epothilone D. Tubulin assembly measurements indicate these bridged epothilone analogues to be mildly active, but without significant microtubule stabilization capacity. Molecular mechanics and DFT energy evaluations suggest the mild activity of the bridged epo-analogues may be due to internal conformational strain.     

Spatial correlations of pairing collective states

The properties of the low-energy nuclear spectrum are greatly affected by pairing correlations. We study these effects in the nucleus ²¹⁰Pb which has two particles moving outside closed shells. The configuration-mixed wave functions describe the motion of particles which are on the average closer together than they would be if the particles were confined to particular orbitals. Since the energy associated with pairing correlations is much smaller than the Fermi energy the width of the associated probability distribution is determined by the wavelength of single particles moving close to the Fermi surface. Despite the fact that the amplitudes associated with high-lying configurations are small, their net effect is important, typically changing the collectivity of the states by a factor of about two. The results of the microscopic calculations compare well with a semiclassical pairing transition density calculated on the basis of the Thomas-Fermi approximation.     

Cumulant functions in optical coherence theory

Cumulant functions are introduced to describe the statistical state of a radiation field. These functions are simply related to the optical coherence functions but have some interesting features. It is shown that if the cumulant functions of all orders greater than some numberN ₀ vanish then they also vanish for all orders greater than 2. Thermal field is the only field having this property. This property holds whether the field is described by a classical stochastic process or by a quantum density operator. Further the particular operator ordering used in defining these cumulant functions for the quantized field affects only the second order cumulant function. To describe the statistical state of a vector field such as partially polarized or unpolarized radiation, one would need to introduce cumulant tensors.     

Reactions involving selenium metal as an electrophile. The enolate - selenolate transformation

When enolate ions are allowed to react with selenium metal, followed by methyl iodide, the corresponding α-methylselenenyl derivatives are produced in high yield.     

Application of the nuclear field theory to monopole interactions which include all the vertices of a general force

The field treatment is applied to the monopole pairing and monopole particle-hole interactions in a two-level model. All the vertices of realistic interactions appear, and the problems treated here have most of the complexities of real nuclei. Yet, the model remains sufficiently simple, so that a close comparison with the results of a (conventional) treatment in which only the fermion degrees of freedom are considered is possible. The applicability to actual physical situations appears to be feasible, both for schematic or realistic forces. The advantage of including the exchange components of the interaction in the construction of the phonon is discussed.