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8 result(s) for "Artyushin, O. I."
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Conjugates of 3,5-Bis(arylidene)-4-piperidone and Sesquiterpene Lactones Have an Antitumor Effect via Resetting the Metabolic Phenotype of Cancer Cells
In recent years, researchers have often encountered the significance of the aberrant metabolism of tumor cells in the pathogenesis of malignant neoplasms. This phenomenon, known as the Warburg effect, provides a number of advantages in the survival of neoplastic cells, and its application is considered a potential strategy in the search for antitumor agents. With the aim of developing a promising platform for designing antitumor therapeutics, we synthesized a library of conjugates of 3,5-bis(arylidene)-4-piperidone and sesquiterpene lactones. To gain insight into the determinants of the biological activity of the prepared compounds, we showed that the conjugates of 3,5-bis(arylidene)-4-piperidone and sesquiterpene lactones, which are cytotoxic agents, demonstrate selective activity toward a number of tumor cell lines with glycolysis-inhibiting ability. Moreover, the results of molecular and in silico screening allowed us to identify these compounds as potential inhibitors of the pyruvate kinase M2 oncoprotein, which is the rate-determining enzyme of glycolysis. Thus, the results of our work indicate that the synthesized conjugates of 3,5-bis(arylidene)-4-piperidone and sesquiterpene lactones can be considered a promising platform for designing selective cytotoxic agents against the glycolysis process, which opens new possibilities for researchers involved in the search for antitumor therapeutics among compounds containing piperidone platforms.
Mechanism of Formation of N-Methyl-N-2-(diphenylphosphoryl)-ethylamide of (Diphenylphosphoryl)acetic Acid
The mechanism of formation of N -methyl-2-(diphenylphosphoryl)acetamide was studied by DFT. The first stage, the reaction of trichlorophosphine with 2-(diphenylphosphoryl)acetic acid, involves three elementary steps, and the explicit inclusion of solvent makes it possible to reduce the activation energy of each of them. The second stage, the reaction of 2-(diphenylphosphoryl)acetyl chloride with a phosphoryl-substituted amine, involves one elementary step.
The first example of a ring closing metathesis in a series of anthracycline antibiotics
A ring-closing metathesis giving 3-pyrroline ring in a series of anthracycline antibiotics on the example of N , N -diallyl derivative of daunorubicin using the first and the second generation Grubbs catalysts was reported. The suggested approach can be used to synthesize new anthracycline anticancer agents.
Preparative scalable method for the synthesis of cyclic and acyclic acetals of chloropropiolaldehyde and their transformation into acetals of lithiumpropiolaldehyde
A simple two-step and easily scalable method for the synthesis of cyclic and acyclic acetals of chloropropiolaldehyde was developed. They readily reacted with n -butyllithium to give stable crystalline acetals of lithiumpropiolaldehyde, which, being strong nucleophiles, reacted with chlorotrimethylsilane, chlorotrimethylstannane, and methyl chloroformate to form bifunctional acetylenes in high yields.
Synthesis of conjugates of sesquiterpene lactones with 3,5-bis(arylidene)piperidin-4-ones as potential NF-κB modulators using phase transfer catalysis conditions
A simple method for modifying sesquiterpene lactones with 3,5-bis(arylidene)piperi-din-4-ones using the phase-transfer catalytic aza-Michael addition in the MeCN—K 2 CO 3 system was developed. Molecular docking revealed that the synthesized conjugates of isoalantolactone, alantolactone, and dehydrocostus lactone with various bis(arylidene)-piperidones directly interact with the DNA binding site of the p50 subunit of nuclear factor κB, which may be indicative of their ability to induce apoptotic death of the tumor cells due to activation of the death receptor expression and, thereby, to exhibit an antitumor effect.
Design of New Daunorubicin Derivatives with High Cytotoxic Potential
Chemotherapy with anthracycline antibiotics is a common method of treating tumors of various etiologies. To create more highly effective cytostatics based on daunorubicin, we used the method of reductive amination using polyalkoxybenzaldehydes. The obtained derivatives of the anthracycline structure have much greater cytotoxicity compared to daunorubicin due to increased affinity for DNA, the ability to disrupt the cell cycle, and their inhibition of the glycolysis process, which is confirmed by data from extensive biological studies and the results of molecular modeling.
The analysis of toxic connections content in water by spectral methods
The current state of ecology means the strict observance of measures for the utilization of household and industrial wastes that is connected with very essential expenses of means and time. Thanks to spectroscopic devices usage the spectral methods allow to carry out the express quantitative and qualitative analysis in a workplace and field conditions. In a work the application of spectral methods by studying the degradation of toxic organic compounds after preliminary radiation of various sources is shown. Experimental data of optical density of water at various influences are given.
Phototransformation of naphthalene in water in the presence of modified polypropylene microfibers
Methods of electron absorption and fluorescence spectroscopy are used to investigate degradation of naphthalene in water upon exposure to UV radiation of a KrCl excilamp in the presence of polypropylene microfibers (PMF) modified by TiO 2 and SnO 2 particles. The results obtained demonstrate that the naphthalene concentration is halved in the presence of PMF. This is caused by the naphthalene adsorption on the PMF surface. UV irradiation of the naphthalene–water–PMF system leads to the formation of fluorescing naphthalene photoproducts in water and on the PMF surface. Naphthalene phototransformation products are detected by the chromatography-mass spectrometry method.