A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones

A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones is described. The synthesis was developed on solid phase and was applied to provide a series of analogs in good yield. The key reactions are acylation of a cysteine derivative with 2,4-dichloropyrimidine-5-carbonyl chloride followed by cyclization to generate a 6-arylmethyl-7-carboxamido-2-chloro-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-one, which is further derivatized with an amine to give the desired 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-one.     

Generalized information theory for hints

This paper develops a new uncertainty measure for the theory of hints that complies with the established semantics of statistical information theory and further satisfies all classical requirements for such a measure imposed in the literature. The proposed functional decomposes into conversant uncertainty measures and therefore discloses a new interpretation of the latters as well. By abstracting to equivalence classes of hints we transport the new measure to mass functions in Dempster-Shafer theory and analyse its relationship with the aggregate uncertainty, which currently is the only known functional for the Dempster-Shafer theory of evidence that satisfies the same set of properties. Moreover, the perspective of hints reveals that the standard independence notion in Dempster-Shafer theory called non-interactivity corresponds to an amalgamation of probabilistic independence and qualitative independence between frames of discernment. All results in this paper are developed for arbitrary families of compatible frames generalizing the very specialized multi-variate systems that are usually studied in information theory.     

Platinum-promoted cyclization reactions of amino olefins : II. Regio- and stereoselectivity in the cyclization reactions of C-methyl substituted pent-4-enylamines

The compounds 1-, 2- and 3-methylpent-4 enylamine cyclize, in a reaction medium containing [PtCl₄]^2-, to the corresponding cis- and trans-dimethylpyrrolidines showing marked regio and stereoselectivity effects. The following cyclization reactions are also reported: a) that of hex-4-enylamine which gives a mixture of 2-ethylpyrrolidine and 2-methylpiperidine, b) that of 2,2-dimethylpent-4-enylamine which produces 2,4,4-trimethylpyrrolidine and c) that of 2,2-dimethylhex-4-enylamine which results in the formation of 2-ethyl-4,4-dimethylpyrrolidine and 2-methyl-5,5-dimethylpiperidine.The X-ray crystal structures of trans-[PtCl₂(amine)(Et₃P)] (amine = cis-2, 4-dimethylpyrrolidine and cis-2,3-dimethylpyrrolidine) are reported.     

Relation between vestigial-sideband filtering and pi/2 progressive phase shift

We show that a Gaussian-shaped vestigial-sideband (VSB) return-to-zero (RZ) on-off-keying (OOK) optical signal is essentially a RZ OOK signal with pi/2 progressive phase shift. The reduced intersymbol interference of the VSB signal can be explained as a destructive interference effect. We experimentally demonstrate a method for generating an effective 40-Gbit/s VSB signal without relying on the detuning of an optical filter.     

Generation and detection of 80-Gbit/s return-to-zero differential phase-shift keying signals

Nonlinear polarization rotation between a pump and a probe signal in a highly nonlinear fiber is used as a modulation process to generate 80-Gbit/s return-to-zero differential phase-shift keying signals. Its performance is analyzed and compared with a conventional on-off keying modulated signal.     

Determination of non-homogeneous high-concentration depth distributions using elastic backscattering data

A computer program has been developed by which the depth concentration distribution of a two-element bulk sample can be determined from elastic backscattering data. The presented calculative procedure can be applied to non-homogeneous high concentrations, where the composition variation as a function of depth has to be considered to obtain correct distributions. Two samples with different compositions, nitrogen in titanium and gold in silicon, were analysed with 2MeVH⁺ and He⁺ ions, respectively, to illustrate the versatility of the calculative program.     

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

Selective protein kinase inhibitors have only been developed against a small number of kinase targets. Here we demonstrate that "high-throughput kinase profiling" is an efficient method for the discovery of lead compounds for established as well as unexplored kinase targets. We screened a library of 118 compounds constituting two distinct scaffolds (furan-thiazolidinediones and pyrimido-diazepines) against a panel of 353 kinases. A distinct kinase selectivity profile was observed for each scaffold. Selective inhibitors were identified with submicromolar cellular activity against PIM1, ERK5, ACK1, MPS1, PLK1-3, and Aurora A,B kinases. In addition, we identified potent inhibitors for so far unexplored kinases such as DRAK1, HIPK2, and DCAMKL1 that await further evaluation. This inhibitor-centric approach permits comprehensive assessment of a scaffold of interest and represents an efficient and general strategy for identifying new selective kinase inhibitors.     

Surface morphology changes of graphite irradiated with energetic helium ions

Implantation of helium ions into graphite has been found to produce surface features, which are discussed in terms of radiation damage as a function of depth into the material. Annealing and electron microscope studies show these surface features to be still well defined after annealing at 1500°C. The suggested interpretation is consistent with the large surface stress found in the surface layers of implanted materials.