NKT cell-dependent glycolipid–peptide vaccines with potent anti-tumour activity

It is known that T cells can eliminate tumour cells through recognition of unique or aberrantly expressed antigens presented as peptide epitopes by major histocompatibility complex (MHC) molecules on the tumour cell surface. With recent advances in defining tumour-associated antigens, it should now be possible to devise therapeutic vaccines that expand specific populations of anti-tumour T cells. However there remains a need to develop simpler efficacious synthetic vaccines that possess clinical utility. We present here the synthesis and analysis of vaccines based on conjugation of MHC-binding peptide epitopes to α-galactosylceramide, a glycolipid presented by the nonpolymorphic antigen-presenting molecule CD1d to provoke the stimulatory activity of type I natural killer T (NKT) cells. The chemical design incorporates an enzymatically cleavable linker that effects controlled release of the active components in vivo. Chemical and biological analysis of different linkages with different enzymatic targets enabled selection of a synthetic vaccine construct with potent therapeutic anti-tumour activity in mice, and marked in vitro activity in human blood.     

Vibration Spectroscopy Stability Investigation of 12-Tungstosilicic Acid Solution

Heteropoly acids (HPA) attract the attention of large variety of scientists, due to HPA’s extraordinary interesting properties and possible application fields. 12-tungstosilicic acid (WSiA), the Keggin type HPA, has some promising characteristic to be used in catalytic processes, but with not well-defined stability. Raman spectroscopy was used for in situ analysis of WSiA hydrolysis in detail in a wide pH range of 1–12. Raman spectroscopy is able to give an almost immediate response/spectrum as a representation of the exact profile/composition of the solution. This method and FTIR spectroscopy, as a complementary technique, enabled recording of the solid and liquid phases of the same sample under different conditions. Our results confirm that the decomposition pathways of WSiA in solution proceed via the formation of the lacunary monovacant anion at pH > 6.4. This anion is a major constituent in pH range up to 9.5. With further increases in pH this species convert to the trivacant lacunary anion. The total decomposition of the Keggin anion to silicate and tungstate occurs at pH > 11.0. The results of the performed study contribute to understand the behavior of WSiA in the water–methanol solution, as the model system of aqueous-organic system. It is concluded that addition of methanol in aqueous solution of WSiA leads to expansion of the pH region where Keggin anion is stable up to 8.1 and above this pH value, precipitation occurs. The obtained data clarify the stability range of WSiA in both water and water–methanol solutions, as well.     

Advanced Developments in Cyclic Polymers: Synthesis,Applications, and Perspectives

Due to the topological effect, cyclic polymers demonstrate different and unique physical and biological properties in comparison with linear counterparts having the same molecular-weight range. With advanced synthetic and analytic technologies, cyclic polymers with different topologies, e.g. multicyclic polymers, have been reported and well characterized. For example, various cyclic DNA and related structures, such as cyclic duplexes, have been prepared conveniently by click chemistry. These types of DNA have increased resistance to enzymatic degradation and have high thermodynamic stability, and thus, have potential therapeutic applications. In addition, cyclic polymers have also been used to prepare organic–inorganic hybrids for applications in catalysis, e.g. catalyst supports. Due to developments in synthetic technology, highly pure cyclic polymers could now be produced in large scale. Therefore, we anticipate discovering more applications in the near future. Despite their promise, cyclic polymers are still less explored than linear polymers like polyolefins and polycarbonates, which are widely used in daily life. Some critical issues, including controlling the molecular weight and finding suitable applications, remain big challenges in the cyclic-polymer field. This review briefly summarizes the commonly used synthetic methodologies and focuses more on the attractive functional materials and their biological properties and potential applications.     

Effect of Support on Catalytic Properties of Platinum-Containing Catalysts in Hydrogenation of a Biphenyl–Diphenylmethane Eutectic Mixture

Russian Journal of Applied Chemistry - Pt/Sup catalysts with SiO2, MCM-48, and Al2O3 supports (Sup) were prepared. The catalysts were studied by methods of low-temperature nitrogen adsorption,...     

Some Transformations of 3-(2,2-Dimethyltetrahydro-2H-pyran-4-yl-2-thioxo-2,3-dihydro-1H-spiro(benzo[h]quinazoline-5,1'-cycloheptan)-4(6H)-one

Russian Journal of Organic Chemistry - Starting from 3-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-2-thioxo-2,3-dihydro-1H-spiro(benzo[h]quinazoline-5,1'-cycloheptan)-4(6H)-one, a series of...     

Green and Catalyst-Free Synthesis of Some New Benzo[4,5]imidazo[1,2-a]pyrimidine Derivatives as Antimicrobial and Antitubercular Agents

Russian Journal of Organic Chemistry - A new series of 4-(1H-imidazol-4-yl)-2-(substituted phenyl)-1,4-dihydrobenzo[4,5]imidazo[1,2-a]­pyrimidines have been synthesized via a one-pot reaction...     

Convenient Microwave-Assisted Chlorosulfonic Acid-Catalyzed Synthesis of Some Quinazolinones from 2-Phenylindole

Russian Journal of Organic Chemistry - A new convenient method has been developed for the synthesis of quinazolinones from 2-phenyl-1H-indole and substituted amines under catalysis by...     

Comparison of the Reactivities of Tyrosine–Proline-Based Dipeptides toward Acylation with Nitrophenyl Benzoates

Russian Journal of Organic Chemistry - The reactivities of the L-Tyr–L-Pro dipeptide and its analog with a hydroxymethyl group instead of carboxy group in the proline moiety were compared by...