Synthesis, Bacteriostatic and Anticancer Activity of Novel Phenanthridines Structurally Similar to Benzo[c]phenanthridine Alkaloids.

In this study, we report the synthesis, antibacterial and anticancer evaluation of 38 novel phenanthridines that were designed as analogs of the benzo[]phenanthridine alkaloids. The prepared phenanthridines differ from the benzo[]phenanthridines in the absence of a benzene A-ring. All novel compounds were prepared from 6-bromo-2-hydroxy-3-methoxybenzaldehyde in several synthetic steps through reduction of Schiff bases and accomplished by radical cyclization.

Study of 2-aminoquinolin-4(1H)-one under Mannich and retro-Mannich reaction.

2-Aminoquinolin-4(1H)-one was reacted with various primary/secondary amines and paraformaldehyde under Mannich reaction conditions. In the case of secondary amines, the reaction in N,N-dimethylformamide yielded expected Mannich products accompanied with 3,3'-methylenebis(2-aminoquinolin-4(1H)-one). Except these main products, the pyrimido[4,5-b]quinolin-5-one derivative was also identified as co-product.

RP-HPLC determination of dissociation constant using solely aqueous mobile phase.

The proposed HPLC method using solely or nearly 100% aqueous mobile buffer as mobile phase offers fast determination of dissociation constant for compounds in relatively wide range of lipophilicity (log P from -2.26 to 2.26).

7-(2-Thienyl)-7-Deazaadenosine (AB61), a New Potent Nucleoside Cytostatic with a Complex Mode of Action.

7-(2-Thienyl)-7-deazaadenosine (AB61) showed nanomolar cytotoxic activities against various cancer cell lines but only mild (micromolar) activities against normal fibroblasts. The selectivity of AB61 was found to be due to inefficient phosphorylation of AB61 in normal fibroblasts. The phosphorylation of AB61 in the leukemic CCRF-CEM cell line proceeds well and it was shown that AB61 is incorporated into both DNA and RNA, preferentially as a ribonucleotide.

Fluorescence properties of selected benzo[c]phenanthridines.

The fluorescence properties of selected benzo[c]phenanthridines (BPs) were examined. The effect of structure, pH and solvent on the fluorescence properties has been investigated. It was found out that the presence of charged iminium nitrogen significantly decreased the fluorescence of the compounds.

Purine scaffold effect on fluorescence properties of purine-hydroxyquinolinone bisheterocycles.

The fluorescence properties of bisheterocyclic compounds that contain purine and the 3-hydroxyquinolin-4(1H)-one skeleton connected with an aliphatic spacer of a different length/structure (3HQP) were examined. It was found that the introducing of the spacer-purine scaffold led in the comparison to 3HQs themselves to (1) the possibility of the effectual excitation in the wider range of excitation wavelengths, moreover, some derivatives can be excited at relatively high wavelengths around 400 nm, (2) the lowering of the quantum yield and (3) the slight longer wavelength shift of the dual emission spectra. Tested organic solvents did not affect significantly the 3HQP fluorescence properties.

Application of wet effluent diffusion denuder for measurement of uptake coefficient of gaseous pollutants.

The comparison of theoretical approaches describing the collection of analyte in the cylindrical wet effluent diffusion denuder (CWEDD) with experimental data is presented. Various absorption liquids were tested for the collection of formaldehyde (distilled-deionized water, H(2)SO(4) solution), acetaldehyde (distilled-deionized water) and nitrous acid (distilled-deionized water, sodium carbonate and sodium bicarbonate solutions of various concentrations and sodium phosphate pH 6-8) in CWEDD. pH of absorption liquids significantly influences the collection of formaldehyde as well as nitrous acid.

Flow-injection chemiluminescence determination of formaldehyde in water.

A modification of the Trautz-Schorigin reaction into a flow-injection analysis configuration is described. Different approaches were used at the optimization of chemiluminescence determination of formaldehyde in water based on the reaction of formaldehyde, gallic acid and hydrogen peroxide in an alkaline solution. Detection system with a 218microl chemiluminescence cell was optimized by both a one-variable-at-a-time method, and a modified simplex method.