Outer membrane vesicles (OMVs), produced by nonpathogenic Gram-negative bacteria, have potentially useful biotechnological applications in extraterrestrial extreme environments. However, their biological effects under the impact of various stressors have to be elucidated for safety reasons. In the spaceflight experiment, model biofilm kombucha microbial community (KMC) samples, in which was a dominant community-member, were exposed under simulated Martian factors (i.
View Article and Find Full Text PDFFour novel Pd and Pt mononuclear π-coordination compounds with general formula [M(HL)Cl], M=Pd, Pt have been synthesized by reaction of [PdCl], [PtCl] anions with N-allyl-4-morpholinethiocarboxamide (HL) and N-Allyl-N'-tert-butylthiourea (HL). All complexes have been characterized by single-crystal X-ray diffraction study and H, C NMR spectroscopy. Cytotoxic, cytostatic and proapoptotic activities of compounds have been determined in vitro on HeLa cell line and compared with cisplatin as etalon drug.
View Article and Find Full Text PDFNucleosides Nucleotides Nucleic Acids
April 2016
This paper presents the results of synthesis and study of cytotoxicity and the anti-adenoviral activity of new N4-derivatives of 6-azacytidine and its α-L-glycopyranosyl analogues obtained by the simplified one-pot version of the silyl condensation method. The resulting acylated 4-methylmercapto-1,2,4-triazin-3(2Н)-one glycosides then underwent the amination and/or ammonolysis to provide 6-azacytidine glycoside analogues (2-6, 12, 15, 17) and compounds with modifications at both base and sugar fragments (11, 15). The evaluation of cytotoxicity and antiviral activity of new compounds against AdV5 showed high selectivity indexes for N4-methyl-6-azacytidine (2) and N,O-tetraacetyl-6-azacytidine (8).
View Article and Find Full Text PDFCoordination and organoelement compounds are rarely proposed as the drug candidates despite their vast potential in the area owing to their strictly controlled geometry and rather extensive surface. This is the first example of the inhibition of transcription in the system of T7 RNA polymerase by cage metal complexes. Their IC50 values reach as low as the nanomolar range, placing them among the most potent metal-based transcription inhibitors.
View Article and Find Full Text PDFA number of new hybrid heteroaromatic compounds, consisting of tricyclic fragments (acridone, thioxanthone and phenazine) and bicyclic fragments (benzimidazole, benzothiazole and benzoxazole) were synthesized using the method, developed by the authors. As a result of screening against the transcription model system of the phage T7 DNA-dependent RNA polymerase three effective inhibitors of the RNA syntheses with the IC50 value of 8.9, 5.
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