Synthesis of Pyrano[2,3-d]pyrimidine-2,4-diones and Pyridino[2,3-d]pyrimidine-2,4,6,8-tetraones: Evaluation Antitumor Activity

A series of some novel pyrano[2,3-d]pyrimidine 4 – 10 with 75–95% yields and pyridino[2,3-d]pyrimidine derivatives 11 – 16 with 75–92% yields is reported. The building structures have been achieved by reaction of 5-arylidene barbituric acid 2 and active nucleophile carbon or nitrogen as examples barbituric acid and acetyl acetone or refluxing of bispyrimidine-2,4,6-trione derivative 3 with cyclizing reagents such as phosphorous pentoxide, hydrazine hydrate and aminothiazole. The newly synthesized structures have been elucidated on the basis of their spectral analysis. Some selected members were screened for antitumor activity. Among the screened compounds 9 , 16 , 7 , 10 and 8 exhibited high antitumor activity.     

5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation

A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, ¹H-NMR, and ¹³C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.     

1,2,4‐Triazine Chemistry Part IV: Synthesis and Chemical Behavior of 3‐Functionalized 5,6‐Diphenyl‐1,2,4‐triazines towards Some Nucleophilic and Electrophilic Reagents

The synthesis and chemical behavior of 3‐functionalized 5,6‐diphenyl‐1,2,4‐triazines towards some electrophilic and nucleophilic reagents are reviewed. The synthesis, unique features, and medicinal, pharmacological, and biological significance of these constituents are also reported.     

Bis(2-sulfanylethyl)amino native peptide ligation

The reaction of a peptide featuring a bis(2-sulfanylethyl)amino (SEA) group on its C-terminus with a cysteinyl peptide in water at pH 7 and 37 °C leads to the chemoselective and regioselective formation of a native peptide bond. This method called SEA ligation enriches the native peptide ligation repertoire available to the peptide chemist. Preparation of an innovative solid support which allows the straightforward synthesis of peptide SEA fragments using standard Fmoc/tert-butyl solid phase peptide synthesis procedures is also described.     

Methoxyperylene bisimides and perylene lactame imides: novel, red fluorescent dyes

The synthesis of methoxyperylene bisimides and perylene lactame imides with aliphatic N-substituents is described. Both classes of dyes exhibit fluorescence in the bathochromic region of visible light so that red light is obtained. The lightfastness of the dyes is very high, thus, there is special interest for diverse applications.     

Interpreting the catalytic voltammetry of an adsorbed enzyme by considering substrate mass transfer, enzyme turnover, and interfacial electron transport

Redox active enzymes can be adsorbed onto electrode surfaces to catalyze the interconversion of oxidized and reduced substrates in solution, driven by the supply or removal of electrons by the electrode. The catalytic current is directly proportional to the rate of enzyme turnover, and its dependence on the electrode potential can be exploited to define both the kinetics and thermodynamics of the enzyme's catalytic cycle. However, observed electrocatalytic voltammograms are often complex because the identity of the rate limiting step changes with the electrode potential and under different experimental conditions. Consequently, extracting mechanistic information requires that accurate models be constructed to deconvolute and analyze the observed behavior. Here, a basic model for catalysis by an adsorbed enzyme is described. It incorporates substrate mass transport, enzyme kinetics, and interfacial electron transport, and it accurately reproduces experimentally recorded voltammograms from the oxidation of NADH by subcomplex Ilambda (the hydrophilic subcomplex of NADH:ubiquinone oxidoreductase), under a range of conditions. Mass transport is imposed by a rotating disk electrode and described by the Levich equation. Interfacial electron transport is controlled by the electrode potential and characterized by a dispersion of rate constants, according to the model of Léger and co-workers. Here, the Michaelis-Menten equation is used for the enzyme kinetics, but our methodology can also be readily applied to derive and apply analogous equations relating to alternative enzyme mechanisms. Therefore, our results are highly relevant to the interpretation of electrocatalytic voltammograms for adsorbed enzymes in general.     

Riemann surfaces defined over the reals

The known (explicit) examples of Riemann surfaces not definable over their field of moduli are those with that field being a subfield of the reals but which cannot be defined over the reals. In this paper we provide explicit families of Riemann surfaces which are definable over the reals but cannot be defined over the field of moduli.     

Quantumness Measures for a System of Two Qubits Interacting with a Field in the Presence of the Time-Dependent Interaction and Kerr Medium

In this work, we introduce the standard Tavis-Cummings model to describe two-qubit system interacting with a single-mode field associated to power-law (PL) potentials. We explore the effect of the time-dependent interaction and the Kerr-like medium. We solve the Schrödinger equation to obtain the density operator that allows us to investigate the dynamical behaviour of some quantumness measures, such as von Neumann entropy, negativity and Mandel’s parameter. We provide how these entanglement measures depend on the system parameters, which paves the way towards better control of entanglement generation in two-qubit systems. We find that the enhancement and preservation of the atoms-field entanglement and atom-atom entanglement can be achieved by a proper choice of the initial parameters of the field in the absence and presence of the time-dependent interaction and Kerr medium. We examine the photons distribution of the field and determine the situations for which the field exhibits super-poissonian, poissonian or sub-poissonian distribution.     

A novel integrated method realizing iteratively optimized modeling for proximity field patterning nanolithography

Processing methods used in photonics and nanotechnology have many limitations hindering the ability to realize devices and restricting the actual number of applications. An ideal processing method should require low-cost equipment, be able to produce very fine details, and be scalable to process large area specimens in an acceptable amount of time. Proximity field nanopatterning (PnP) is a lithography method possessing these features. By using interference patterns produced by a two-dimensional phase mask, the technique is able to generate a submicron detailed exposure on a millimeter-size slab of light sensitive photopolymer, which is then developed like a photographic plate to reveal three-dimensional interference patterns from the phase mask. While it is possible to use computer aided simulations to obtain the interference patterns produced by a mask with a certain pattern, the inverse problem of producing a mask for a desired interference pattern cannot be solved in the same way due to the intricacies of light interactions involved in producing the final interference pattern. An alternative method is to iteratively optimize the phase mask so that the interference patterns obtained converge to the desired pattern. The method is elaborated in this article.     

Practical and reliable synthesis of dialkyl N-arylphosphoramidates with nitroarenes as substrates

A new single-step transformation of readily available nitroarenes with trialkyl phosphites, which can be performed both under thermal and microwave conditions, delivers dialkyl N-arylphosphoramidates in good yields and short reaction times.