N-vinyl carbazole copolymers

The synthesis of N-vinyl carbazole (VCbz) copolymers, some of which contain electron-accepting groups, is described. The new copolymers are: copoly[N-vinyl carbazole-di(2-N-carbazylethyl)-fumarate](II); copoly(N-vinyl carbazole-vinyl-2,4-dinitrobenzene-sulfonate)(IV); copoly(N-vinyl carbazole-vinyl-2,4-dinitrobenzene-sulfenate)(V); copoly(n-butyl acrylate-t-butyl peracrylate)(VII); copoly(n-butyl acrylate-t-butyl acrylate-graft-N-vinyl carbazole)(VIII).     

Chemometric outlook on correlations between retention parameters of polar and semipolar HPLC columns and physicochemical characteristics of ampholytic substances of biological and pharmaceutical relevance

The Quantitative Property-Retention Relation (QPRR) approach was applied to analyze the correlations between the retention parameters of ampholytic, biologically active substances and their physicochemical (predicted/spectral) characteristics. The retention parameters were obtained for polar and semipolar HPLC columns at various compositions of mobile phases and pH conditions. These values are a unique collection of chromatographic parameters that are a measure of lipophilicity and, consequently, can be very helpful in assessing pharmacological potency of the compounds investigated. Three QPRR models that meet the predictive capability criteria were developed. The relationships can be used to gain pharmacologically interesting information on the biologically active ampholytic substances.

     

DNA condensation and interaction with zwitterionic phospholipids mediated by divalent cations

Artificial viruses are considered to be a promising tool in gene therapy. To find lipid-DNA complexes with high transfection efficiency but without toxicity is a fundamental aim. Although cationic lipids are frequently toxic for cells, neutral lipids are completely nontoxic. Zwitterionic lipids do not interact with DNA directly; however, the interaction can be mediated by divalent cations. Langmuir monolayers represent a well-defined model system to study the DNA-lipid complexes at the air/water interface (quasi-2D systems). In this work, isotherms, infrared reflection absorption spectroscopy (IRRAS), X-ray reflectivity (XR), grazing incidence X-ray diffraction (GIXD), and Brewster angle microscopy (BAM) measurements are used to study the interaction of calf thymus DNA with DMPE (1,2-dimyristoyl-phosphatidylethanolamine) monolayers mediated by Ca2+ or Mg2+ ions. DNA adsorption is observed only in the presence of divalent cations. At low lateral pressure, the DNA partially penetrates into the lipid monolayer but is squeezed out at high pressure. The adsorption layer has a thickness of 18-19 A. Additionally, GIXD provides information about a one-dimensional ordering of adsorbed DNA. The periodic distance between DNA strands depends on the type of the divalent cation.     

Photoconductive copolymers containing N-vinylcarbazole

The synthesis of N-vinylcarbazole (VCbz) copolymers in which electron-accepting groups are incorporated into the polymer chain is reported. The acceptors were introduced by appropriate reactions of VCbz–vinyl acetate or VCbz–acryloyl chloride copolymers and consisted of 3,5-dinitrobenzoyl, 2,4-dinitrophenyl acrylate, β-2,4-dinitrophenoxy propionate, and trichlorobenzoquinone units. The copolymer containing the 3,5-dinitrobenzoyl units required no chloranil as a dopant to be photoconductive, and in fact showed a slightly improved photoresponse relative to conventional poly VCbz doped with external chloranil.     

Modeling of Anticancer Sulfonamide Derivatives Lipophilicity by Chemometric and Quantitative Structure-Retention Relationships Approaches

Sulfonamides are a classic group of chemotherapeutic drugs with a broad spectrum of pharmacological action, including anticancer activity. In this work, reversed-phase high-performance liquid chromatography and biomimetic chromatography were applied to characterize the lipophilicity of sulfonamide derivatives with proven anticancer activities against human colon cancer. Chromatographically determined lipophilicity parameters were compared with obtained logP, employing various computational approaches. Similarities and dissimilarities between experimental and computational logP were studied using principal component analysis, cluster analysis, and the sum of ranking differences. Furthermore, quantitative structure–retention relationship modeling was applied to understand the influences of sulfonamide’s molecular properties on lipophilicity and affinity to phospholipids.