Dimethylsilane polyamines: cytostatic compounds with potentials as anticancer drugs

Several dimethylsilane tetramines [homologs of spermine with an Si(CH3)2 group in the central carbon chain], a carbon analog of the dimethylsilane tetramines [containing C(CH3)2 instead of Si(CH3)2] and a dimethylsilane hexamine were studied with regard to their cytotoxic activity and their ability to interact with double-stranded DNA. All polyamine analogs exerted cytostatic effects to several cell lines at micromolar concentrations. Their ability to condense DNA was comparable to and their ability to displace ethidium bromide from binding to DNA was superior to that of spermine. Their cytostatic effect was not correlated with the depletion of cellular spermidine concentrations. It is suggested that the new polyamine analogs act mainly by displacing spermidine from binding sites which are essential for the promotion of cell growth.     

Spectroscopic and electrical properties of 3-alkyl pyrrole-pyrrole copolymers

Three types of copolymers composed of pyrrole and 3-alkyl pyrroles (with alkyl being pentyl, nonyl and undecyl) have been synthesized. A strong linear dependency of the alkyl chain length on the as-prepared copolymer physical properties is demonstrated via (a) DSC (for phase transition temperatures and enthalpy changes) and (b) UV-vis (for wavelengths of the polaronic and bipolaronic electronic transitions, and ratio of the corresponding absorbances). A trend in the copolymers' doping level vs alkyl chain length is also estimated, via IR, by taking the ratio of band intensities of the stretching modes of the polaronic and bipolaronic species. The copolymers are found to be soluble in organic solvents and their solutions can be cast onto glass substrates or metals resulting in thin films, which can be used as the electroactive component of Schottky diodes. The electrical properties of these diodes are also found to be dependent on increasing 3-alkyl chain length.     

Quantum non-demolition measurements using cold atoms in an optical cavity

Abstract

In this paper we present a theoretical analysis of a recent quantum non-demolition experiment in optics using cold atoms in a magneto-optical trap as a nonlinear medium. A signal beam and a meter beam from two independent lasers are coupled within a A-type three-level scheme in the D1 line of ⁸⁷Rb atoms. The experimental results for the relevant quantum correlations of the fields represent up to now the best achievement for a single back-action evading measurement. Moreover, they are found to be in remarkably good agreement with the theoretical predictions from a fully quantum model for three-level atoms in a doubly resonant cavity.     

Austenite Grain Growth in a 2.25Cr-1Mo Vanadium-Free Steel Accounting for Zener Pinning and Solute Drag: Experimental Study and Modeling

Metallurgical and Materials Transactions A - Austenite grain size has been experimentally determined for various austenitization temperatures and times in a 2.25Cr-1Mo vanadium-free steel. Three...     

The formation of intermetallics in dissimilar Ti6Al4V/copper/AISI 316 L electron beam and Nd:YAG laser joints

The welds of titanium alloys with steels suffer from the brittleness of resulting intermetallic compounds. In present study, we report the feasibility of Ti6Al4V to stainless steel AISI 316L welding through pure copper interlayer carried out by electron beam and pulsed Nd:YAG laser. The nature and the localization of intermetallic phases in these welds have been studied by SEM, EDS, XRD and microhardness measurements. The simplified scenario of weld formation has been proposed in order to understand the mechanism of weld formation and to explain the way local phase content determines the mechanical properties.It can be concluded that the insertion of 500 μm pure copper interlayer allows reducing but not suppressing the formation of brittle Ti–Fe and Ti–Cr-based phases. The local accumulation of Cu–Ti and Cu–Fe–Ti-based phases is less detrimental to the strength of the welds, which makes joining possible. The thickness of brittle regions is reduced due to short lifetime of the melt and compensated by the ductilizing effect of copper. The tensile strength of the welds is limited by brittleness of CuTi₂ + FeTi + α-Ti layer situated next to the solid Ti6Al4V.     

Polypropylene composites obtained from self‐reinforced hybrid fiber system

The purpose of the study was to obtain a composite material with the self‐reinforced structure, which processing provide increased mechanical properties. The composites used in presented work were prepared from the two types of fiber mixtures, both were based on polypropylene fibers, the difference was in used cellulose or wood flour filler. Composites were prepared using the hot compaction method. The presented research describes the effect of the composite composition and processing conditions. The results include the static tension measurements, tensile impact tests and thermal analysis, including: DSC and DMTA. The structure has been studies using the SEM observations. Results of presented studies confirm the self‐reinforcing effect in obtained hybrid composites. It provides in the comparison to the standard wood polymer composites to the higher level of material reinforcement with lower amount of natural filler. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133, 43283.     

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach

Starting from suvorexant (trade name Belsomra), we successfully identified interesting templates leading to potent dual orexin receptor antagonists (DORAs) via a scaffold‐hopping approach. Structure–activity relationship optimization allowed us not only to improve the antagonistic potency on both orexin 1 and orexin 2 receptors (Ox1 and Ox2, respectively), but also to increase metabolic stability in human liver microsomes (HLM), decrease time‐dependent inhibition of cytochrome P450 (CYP) 3A4, and decrease P‐glycoprotein (Pgp)‐mediated efflux. Compound 80 c [{(1S,6R)‐3‐(6,7‐difluoroquinoxalin‐2‐yl)‐3,8‐diazabicyclo[4.2.0]octan‐8‐yl}(4‐methyl‐[1,1′‐biphenyl]‐2‐yl)methanone] is a potent and selective DORA that inhibits the stimulating effects of orexin peptides OXA and OXB at both Ox1 and Ox2. In calcium‐release assays, 80 c was found to exhibit an insurmountable antagonistic profile at both Ox1 and Ox2, while displaying a sleep‐promoting effect in rat and dog models, similar to that of the benchmark compound suvorexant.