Stable Bicyclic Functionalized Nitroxides: The Synthesis of Derivatives of Aza-nortropinone-5-Methyl-3-oxo-6,8-diazabicyclo[3.2.1]-6-octene 8-oxyls.

In recent decades, bicyclic nitroxyl radicals have caught chemists' attention as selective catalysts for the oxidation of alcohols and amines and as additives and mediators in directed C-H oxidative transformations. In this regard, the design and development of synthetic approaches to new functional bicyclic nitroxides is a relevant and important issue. It has been reported that imidazo[1,2-]isoxazoles formed during the condensation of acetylacetone with 2-hydroxyaminooximes having a secondary hydroxyamino group are recyclized under mild basic catalyzed conditions to 8-hydroxy-5-methyl-3-oxo-6,8-diazabicyclo[3.

Synthesis, Anticancer, and Antibacterial Activity of Betulinic and Betulonic Acid C-28-Triphenylphosphonium Conjugates with Variable Alkyl Linker Length.

Background: Conjugation of triterpenoids such as betulinic acid 1 with the Triphenylphosphonium (TPP) group is a powerful approach to generating medicinal compounds. Their development proposes structure optimization in respect of availability and activity towards target cells and organelles. Selection of 1 or its precursor betulonic acid 2 and the optimal linker is of particular importance for drug candidate identification among the TPP-triterpenoid conjugates.

Design, Synthesis, and Cancer Cell Growth Inhibitory Activity of Triphenylphosphonium Derivatives of the Triterpenoid Betulin.

A series of new triphenylphosphonium (TPP) derivatives of the triterpenoid betulin (1, 3-lup-20(29)-ene-3β,28-diol) have been synthesized and evaluated for cytotoxic effects against human breast cancer (MCF-7), prostate adenocarcinoma (PC-3), vinblastine-resistant human breast cancer (MCF-7/Vinb), and human skin fibroblast (HSF) cells. The TPP moiety was applied as a carrier group through the acyl linker at the 28- or 3- and 28-positions of betulin to promote cellular and mitochondrial accumulation of the resultant compounds. A structure-activity relationship study has revealed the essential role of the TPP group in the biological properties of the betulin derivatives produced.

[Studies of the biological age in adult taiga ticks Ixodes persulcatus (Ixodinae)].

The history of studies of the biological age in ixodid ticks is discussed. A method of estimation of the biological age in adult ticks of the genus Ixodes by the degree of fat inclusions in midgut cells and in the fat body is developed. An "age scale" for the determination of the calendar age was assumed.

[The connection of polymorphism I/D of the gene angiotensin-converting ferment and D442G gene of protein-carrier of cholesterol ethers with atherosclerosis risk factors in patients of elderly and senile age with coronary heart disease in the Republic Sakha (Yakutia)].

The authors analyse allocation of genotypes frequencies of polymorphism I/D of the gene of angiotensin-converting ferment (ASYA) and D442G gene of protein-transmitting agent of cholesterol ethers (CETP) in patients of elderly, senile age and long-livers with coronary heart disease taking into account their nationality, age and sex. With the age, the frequency reduction of occurrence of genotype ACE*I/*I has been observed and there is a tendency to increase of genotype frequency ACE*D/*D. Sexual distinctions in frequency of revealing of homozygous genotype ACE*D/*D have been revealed at the relative analysis of genotypes ACE*D/*D and ACE*D/*I.