Combined use of complexes of the most active chemotherapeutic drugs and detonation nanodiamonds (DND) is a new trend in cancer therapy, which is probably related to selective chemotherapeutic drug delivery by DND to the zone of so-called cancer stem cells (CSC). Stable DND complexes of 4–5 nm size with salinomycin—a strong CSC inhibitor—have been obtained (as a suspension). It has been demonstrated that a complex administration considerably increases the drug antitumor effect on the transplantable tumor of LLC mice. A similar effect has been observed in CSC models in vivo, obtained by exposure of stem cells of normal mice tissues to a carcinogen 1,2-dimethylhydrazine. It has also been found out, that administration of DND complexes with the conditioned medium from mesenchymal stem cells (MSC) cultures to mice results in a considerable stimulation of stem cell pools in normal mice tissues, which can be used in regenerative medicine.
AbstractA variety of functionalized N‐propargylanabasine derivatives, useful precursors of new biologically active anabasine‐based compounds, is synthesized by three‐component condensation reactions of anabazine hydrochloride (I) with paraformaldehyde and terminal alkynes.
Methods for the preparation of fluorinated benzo[d]-isothiazoles, benzo[d]isothiazol-3(2H)-ones and benzo[b]-thiophenes from available 2,4-di- and 2,4,6-trinitrotoluenes are described. One of them entails fluoro- or trifluoroethoxy-denitration of corresponding nitro- or dinitroheterocycles obtained from polynitrotoluenes. An alternative approach is based on a stepwise regioselective substitution of nitro groups in polynitrotoluenes or polynitrobenzoic acid derivatives (amides, nitriles) with S-, O- and F-nucleophiles followed by heterocyclic ring closure. The methods were applied for the conversion of polynitroaromatic compounds to pharmacologically-useful fused heterocycles.
2-Methyltetrahydroanthra[2,3-d]isothiazole-3,5,10-trione and 2-R-tetrahydroanthra[2,1-d]isothiazole-3,6,11-triones were synthesized by the reactions of 3-chloro-9,10-dioxo-9,10-dihydroanthracene-2-carboxamide and 1-nitro-9,10-dioxo-9,10-dihydroanthracene-2-carboxamide with alkanethiols followed by cyclization of the resulting alkylthioamides into isothiazolones under the action of SO2Cl2. The products were oxidized to give the corresponding S-oxides and S,S-dioxides.
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The conjugated nitration of cyclic olefins by NO2BF4 in acetic anhydride, whose course is greatly dependent on the structural features of the olefins undergoing nitration has been studied.
The introduction of the adamantyl radical to the molecule of methacrylates and vinyl esters of carboxylic acids leads to an increase in their polymerizability.