Synthesis of analogs of the phenylamino-pyrimidine type protein kinase C inhibitor CGP 60474 utilizing a Negishi cross-coupling strategy

Analogs of 3-{4-[2-(3-chlorophenylamino)-pyrimidin-4-yl]-pyridin-2-yl-amino}-propanol (CGP 60474) were synthesized as useful models for the evaluation of structure-activity relationships of phenylamino-pyrimidine-type protein kinase C inhibitors. The approach involved Pd-assisted cross-coupling as the key step. Negishi-type coupling was performed both with free amino functionalities and Boc-protected amines present and showed that the protection-cross-coupling-deprotection sequence leads to significantly higher yields.     

Reproductivity for a nematic liquid crystal model

In this paper we prove existence of weak solution with the reproductivity in time property, for a penalized PDE’s system related to a nematic liquid crystal model. This problem is relatively explict when time-independent Dirichlet boundary conditions are imposed for the orientation of crystal molecules. Nevertheless, for the time-dependent case, the treatment of the problem is completely different. The verification of a maximum principle for weak reproductive solutions is fundamental in the argument.     

Effect of dimensional and magnetic quantization hybridization in the optical absorption spectra of nanoheterosystems with <Emphasis Type="Italic">D</Emphasis><Superscript>(−)</Superscript>-states

The magnetoabsorption of light by quantum dot — D^(–)-center complexes synthesized in a transparent dielectric matrix — is theoretically studied with allowance for dispersed quantum dot (QD) sizes. In the effective mass approximation, an analytical expression for the impurity magnetoabsorption coefficient of light polarized in the quantizing magnetic polarization field direction is derived.Translated from Izvestiya Vysshikh Uchebnykh Zavedenii, Fizika, No. 10, pp. 67–72, October, 2004.     

Hyperbolic Harmonic Functions: Weak Approach with Applications in Function Spaces

Harmonic functions with respect to the Poincare metric on the unit ball are called hyperbolic harmonic functions. We establish the weak formulation of hyperbolic harmonic functions and use it in the study of hyperbolic harmonic function spaces. In particular, we give the Carleson measure characterization for the whole spectrum of spaces, whose analytic counterparts include among else Bloch spaces, Bergman-spaces, Besov-spaces, and Q_p-spaces. The second author was supported by the Finnish Cultural Foundation.     

On the existence ofp-units and minkowski units in totally real cyclic fields

LetK be a totally real cyclic number field of degree n > 1. A unit inK is called an m-unit, if the index of the group generated by its conjugations in the group U*_K of all units modulo ±1 is coprime tom. It is proved thatK contains an m-unit for every m coprime to n. The mutual relationship between the existence of m-units and the existence of a Minkowski unit is investigated for those n for which the class number hФ(ζ_n) of the n-th cyclotomic field is equal to 1. For n which is a product of two distinct primes p and q, we derive a sufficient condition for the existence of a Minkowski unit in the case when the field K contains a p-unit for every prime p, namely that every ideal contained in a finite list (see Lemma 11) is principal. This reduces the question of whether the existence of a p-unit and a q-unit implies the existence of a Minkowski unit to a verification of whether the above ideals are principal. As a corollary of this, we establish that every totally real cyclic field K of degree n = 2q, where q = 2, 3 or 5, contains a Minkowski unit if and only if it contains a 2-unit and a q-unit.     

The role of surface and volume defects in the fracture of glass under quasi-static and dynamic loadings

In this paper, the role of surface and volume defects on fracture in soda-lime glass is analyzed when samples are submitted to quasi-static or dynamic loadings. To investigate fracture, different experiments are carried out, namely, quasi-static compression of glass spheres and edge-on-impacts. The first test series aims at studying crack initiation. Different surface treatments are performed to study their influence on the failure load, from which it is concluded that initiation of cracks occurs in the vicinity of the contact surface. The second series is concerned with the examination of crack patterns under dynamic loadings with two different strikers (i.e., soft/flat and hard/perforating projectiles). Crack initiation under dynamic load histories is investigated near and far from the impact zone and it is concluded that it cannot take place within the volume, except in a very small zone close to the impact point. Conversely, initiation of damage from the surface, at a location far from the impact point, is possible and clearly present with a soft projectile.     

The one dimensional anderson model with off diagonal disorder: band centre anomaly

We study theE-dependence of the Lyapounov exponent <(E)> of an electron with energyE in the one dimensional Anderson model with off diagonal disorder. In the neighbourhood of the band centre we find for nonzero disorder E)>log^–1 E0 forE0, but all even moments of Re(E) diverge logarithmically. As the probability of Re (E)=0 decreases to zero forE0 we conclude that the electron is always exponentially localised.     

A novel bis-phenanthridine triamine with pH controlled binding to nucleotides and nucleic acids

The new bis-phenanthridine triamine is characterised by three pK(a) values: 3.65; 6.0 and >7.5. A significant difference in the protonation state of at pH = 5 (four positive charges) and at pH = 7 (less than two positive charges) accounts for the strong dependence of -nucleotide binding constants on nucleotide charge under acidic conditions, whereas at neutral pH all -nucleotide complexes are of comparable stability. All experimental data point at intercalation as the dominant binding mode of to polynucleotides. However, there is no indication of bis-intercalation of the two phenanthridine subunits in binding to double stranded polynucleotides, the respective complexes being most likely mono-intercalative. Thermal stabilisation of calf thymus DNA (ct-DNA) and poly A-poly U duplexes upon addition of is significantly higher at pH = 5 than at neutral conditions. This is not the case with poly dA-poly dT, indicating that the specific secondary structure of the latter, most likely the shape of the minor groove, plays a key role in complex stability. At pH = 5 acts as a fluorimetric probe for poly G (emission quenching) as opposed to other ss-polynucleotides (emission increase), while at neutral conditions this specificity is lost. One order of magnitude higher cytotoxicity of compared to its "monomer" can be accounted for by cooperative action of two phenanthridinium units and the charged triamine linker. The results presented here are of interest to the development of e.g. sequence-selective cytostatic drugs, and in particular for the possibility to control the drug activity properties over binding to DNA and/or RNA by variation of the pH of its surrounding.     

Polymerization of hexamethylcyclotrisiloxane with a biscatecholsiliconate. II. Kinetics of polymerization

The kinetics of polymerization were investigated for the polymerization of hexamethylcyclotrisiloxane (D₃) in toluene with methanol or water as an initiator, benzyltrimethylammonium bis(o-phenylenedioxy)phenylsiliconate as a catalyst, and dimethyl sulfoxide (DMSO) as a promoter. The rate of initiation was found to be comparable with both water and methanol. Addition of catechol drastically reduces the rate of initiation. The rate of propagation was found to be dependent upon the catalyst, DMSO, catechol and the aging of the catalyst solution. Two types of functional groups were postulated to be present during the propagation reaction, i.e., ?SiOH (dormant form) and ?SiONR₄ (living form). The former can be converted to the latter by R₄NOH derived from hydrolysis of catalyst. A postulated mechanism of polymerization with biscatecholsiliconate is presented.