Published in Russian Chemical Bulletin
The deboronation of enantiomers of planar-chiral benzyl (3-formamido-1,2-dicarba-closo-dodecaboran-1-yl)acetate gave the individual (RP)- and (SP)-enantiomers (ee > 98%) of a new amino acid containing a nido-carborane fragment, (3-ammonio-7,8-dicarba-nido-undecaboran-7-yl)acetic acid. Chiral HPLC methods for the analysis of enantiomeric purity of t...
Published in Russian Chemical Bulletin
Nucleophilic substitution of a chlorine atom in 4,5 dichloro-1,2-dithiole-3-thione with per-O-acetyl-1-mercaptho derivatives of d-glucose, d-galactose, d-mannose, d-xylose, l-arabinose, and d-maltose gave six new acetylthioglycoside conjugates of 4-chloro-1,2-dithiole-3-thione. These thioglycosides were shown to possess cancer preventive activity o...
Published in Russian Chemical Bulletin
1-(3-Butyn-1-ylthio)-1,2-dicarba-closo-dodecaborane was synthesized by the alkylation of 1-mercapto-1,2-dicarba-closo-dodecaborane trimethylammonium salt with butyn-3-yl methanesulfonate. The deboronation reaction of this compound gave the corresponding derivative based on nido-carborane, namely, 7-(3-butyn-1-ylthio)-7,8-dicarba-undecaborate anion....
Published in Russian Chemical Bulletin
New 3,5-disubstituted-1,2,4-thiadiazoles were synthesized and together with a series of their analogs obtained earlier were tested for cytotoxic activity to breast adenocarcinoma MCF-7 and lung carcinoma A 549 cells. The selectivity of cytotoxic action was determined in comparison to etiologically noncancerous breast epithelial cells MCF-10A and lu...
Published in Russian Chemical Bulletin
A virtual set of new lactam-containing derivatives of arylsulfonylglycines 1a–d and 2a–d was designed and analyzed using structure–activity computer models (web-services PASS Online, AntiBac-Pred, and GUSAR Acutetoxicity). The antimicrobial activity against Staphylococcus aureus along with low toxicity was predicted for these derivatives. Compounds...
Published in Russian Chemical Bulletin
Five scaffolds (phenoxybenzene, benzofuran, azolobenzimidazole, oxoindole, and uracil), which are promising as sources of compounds with high RAGE inhibitory activity, were found in silico among ten structurally different classes of the synthesized substances using a multitarget neural network model of the dependence of the RAGE inhibitory activity...
Published in Russian Chemical Bulletin
A series of 3,4-diarylpyrrole-2-carboxamides was synthesized using the Barton—Zard reaction of nitrostilbenes with ethyl isocyanoacetate in the key stage. The antiproliferative properties of these compounds were studied on a sea urchin embryo model, as well as on 60 human tumor cell lines.
Published in Russian Chemical Bulletin
A convenient method for the synthesis of 2-(2-R-5-oxo-6,7-dihydro-4H-[1,2,4]triazolo-[1,5-a]pyrimidin-6-yl)acetanilides based on the regioselective domino reaction of N-arylitaconimides with substituted 3-aminotriazoles was proposed. Presumably, the reaction pathway includes the conjugated aza-addition of the endo-nucleophilic center of triazole to...
Published in Russian Chemical Bulletin
A series of new 1,3,4-oxadiazole derivatives bearing the 2-positioned 2,5-dimethoxyphenyl substituent and 5-positioned organylsulfanyl moiety were designed and synthesized. Screening for anticancer activity against an array of human cancer cells revealed the superior activity of 2-(2,5-dimethoxyphenyl)-5-propylthio-1,3,4-oxadiazole. 2-(2,5-Dimethox...
Published in Russian Chemical Bulletin
The influence of exogenous factors on the selectivity of biotransformation of cholesterol 3β-methyl ether by Mycobacterium sp. was studied. The main product of the microbiological transformation was Δ5-dehydroepiandrosterone 3β-methyl ether. The presence of methyl-β-cyclodextrin in the bacterial growth medium led to a change in the ratio of the rea...
