Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioisomers for Antimalarial,Antiproliferative and Antimicrobial Activities

A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate cancer (IC₅₀ = 24 nM) than Puromycin (IC₅₀ = 270 nM) and Doxorubicin (IC₅₀ = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 µM; 9b: MBIC = 100 µM).     

Shape preserving interpolation by cubic G1 splines in $${\mathbb{R}^3}$$

In this paper, G ¹ continuous cubic spline interpolation of data points in , based on a discrete approximation of the strain energy, is studied. Simple geometric conditions on data are presented that guarantee the existence of the interpolant. The interpolating spline is regular, loop-, cusp- and fold-free.      

Direct determination of celiprolol in human urine using on-line coupled ITP-CZE method with fiber-based DAD

The present work illustrated possibilities of column-coupling electrophoresis combined with DAD for the direct quantitative determination of trace drug (celiprolol, CEL) in clinical human urine samples. ITP, on-line coupled with CZE, served as an ideal injection technique (high sample load capacity, narrow and sharp drug zone). Moreover, the ITP provided an effective on-line sample pretreatment (preseparation, purification and preconcentration of the drug) producing analyte zone suitable for its direct detection and quantitation in CZE stage. Spectral DAD in comparison with single wavelength ultraviolet detection enhanced value of analytical information (i) verifying purity (i.e., spectral homogeneity) of drug zone (according to differences in spectrum profiles when compared tested and reference drug spectra) and (ii) indicating zones/peaks with spectra similar to the drug spectrum (potential structurally related metabolites). The characterization of trace analyte signals superposed on the baseline noise was more definite thanks to the application of background correction and smoothing procedure to the raw DAD spectra (producing relevant spectral response). The proposed ITP-CZE-DAD method was characterized by favorable performance parameters for CEL in urine matrices {e.g., the lower limit of quantification was 9.7 ng/mL, RSD and relative error of the determinations were lower than 3% (precision) and 1% (accuracy), respectively, analyte peak exhibited spectral homogeneity (reflecting separation selectivity), separation efficiency was 84,500 theoretical plates} and successfully applied in a trial pharmacokinetic study of CEL.     

Synthesis and Photophysical Properties of 3,6-Diphenyl-9-hexyl-9H-carbazole Derivatives Bearing Electron Withdrawing Groups

3,6-Diphenyl-9-hexyl-9H-carbazole derivatives bearing electron withdrawing groups, such as the formyl or the nitro-group in 4-positions of the phenyl substituents, were prepared and characterized. Their photophysical properties were evaluated and compared with those of the unsubstituted counterpart 3,6-diphenyl-9-hexyl-9H-carbazole. The electron withdrawing groups bearing compounds exhibited considerable red shifts of the absorption and the emission maxima. While 3,6-di(4-nitrophenyl)-9-hexyl-9H-carbazole emitted in the orange region of the visible spectrum with its emission maximum peaking at 585 nm, 3,6-di(4-formylphenyl)-9-hexyl-9H-carbazole gave a pure blue emission with a luminescence quantum yield of 95% peaking at 450 nm. Observed features were explained using quantum mechanical calculations and organic light emitting diodes using the formylphenyl substituted compound as emissive layer were built demonstrating the practical applicability of this class of compounds.     

Sediment extraction and clean-up for organic phosphorus analysis by electrospray ionization tandem mass spectrometry

A method to prepare NaOH sediment extracts for organic P compound analysis with electrospray ionization tandem mass spectrometry (ESI-MS-MS) was developed on natural samples. Ion exchange, rotary evaporation and mass cut-off filtering proved to be suitable for sample preparation. Samples were analyzed with ESI-MS-MS, and reproducibility and repeatability of the method was calculated. In addition, ³¹P-nuclear magnetic resonance spectroscopy (³¹P NMR) was used to measure recovery of different P compound groups such as orthophosphate (Ortho-P), orthophosphate monoesters (Monoester-P), orthophosphate diesters (Diester-P) and pyrophosphates (Pyro-P).

The developed sample preparation method resulted in an easy-to-spray liquid for the ESI-MS-MS instrumentation. The overall P recovery was 65% and ³¹P NMR showed that Diester-P, possibly in the form of DNA, was apparently lost through the filtering step most likely due to their size. Variances in the total intensities of the MS scans (relative standard deviation (R.S.D.) 35–54%) were for about 50% due to repeated MS runs. Covariances of the peaks in the MS spectra were calculated to be for about 30% due to the sample preparation procedure. Finally, with the ESI-MS-MS approach, 11 peaks in the mass spectra were found likely to represent phosphate containing compounds.     

Barycentric coordinates for Lagrange interpolation over lattices on a simplex

In this paper, a (d?+?1)-pencil lattice on a simplex in ${\mathbb{R}}^d$ is studied. The lattice points are explicitly given in barycentric coordinates. This enables the construction and the efficient evaluation of the Lagrange interpolating polynomial over a lattice on a simplex. Also, the barycentric representation, based on shape parameters, turns out to be appropriate for the lattice extension from a simplex to a simplicial partition.     

A New Tool in Metabolism Research—Combination of OPLC On-Line Radioactivity Detection with HPLC—RD Technique

JPC – Journal of Planar Chromatography – Modern TLC - This paper reports a recently developed technique, coupling of optimum-performance laminar chromatography (OPLC) with online...     

Non-local Dirichlet forms generated by pseudodifferential operators on compact abelian groups

Let G_i, 1 ≤ i ≤ n, be compact abelian groups and let Γ_i , 1 ≤ i ≤ n, be countable dual groups. We consider G = G₁ ⊕ G₂ ⊕ … ⊕ G_n and Γ = Γ₁ ⊕ Γ₂ ⊕ … ⊕ Γ_n . For 1 ≤ j ≤ n, let a_j be a negative definite function on Γ_j and a (γ) = . For φ ∈ S (G), the set of all generalized trigonometrical polynomials on G, we define , where (γ) = a_j (γ_j) (γ), 1 ≤ j ≤ n. Then is a Dirichlet form with the domain on L² (G). (© 2008 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim)