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Chemist from RUDN University together with colleagues from the institutes of the Russian Academy of Sciences simplified the synthesis of antitumor compounds
Chemist from RUDN University together with colleagues from the institutes of the Russian Academy of Sciences simplified the synthesis of antitumor compounds
Chemist from RUDN University in collaboration with colleagues from the Institute of organic chemistry named after N. D. Zelinsky and the Institute of developmental biology named after N. K. Koltsova RAS has developed a new method for the synthesis of isoxazole derivatives-substances that destabilize the process of cell division and in the future may become the basis for new anti-cancer drugs. The new method is based on the use of readily available reagents and does not require high temperatures.

Many modern anti-cancer drugs are toxic, difficult to access, and/or very expensive. In addition, tumor cells can develop resistance to the drugs used. Therefore, researchers are studying the biological properties of molecules to obtain new anti-cancer drugs with optimal properties. One of the most common approaches to searching for such drugs is testing analogs of substances with already proven antitumor activity. These substances include, in particular, isoxazole derivatives that inhibit — “turn off” — the hsp90 protein necessary for the survival of tumor cells. However, compounds of this class are not readily available due to the complexity of the synthesis procedure, which requires, in particular, the complete absence of water molecules, and reagents are expensive and toxic.

Viktor Khrustalev, a chemist from RUDN University, and his colleagues have developed a method for synthesizing isomers of these substances, that is, compounds that are identical in atomic composition, but differ in the arrangement of atoms in space. As raw materials, readily available derivatives of aryl nitromethanes and chloroacetamides were used, and the reaction itself was carried out at temperatures of no more than 80 degrees at atmospheric pressure and did not require anhydrous conditions.

The resulting substances had anti-cancer activity, but unlike the prototype compounds, they do not inhibit the Hsp90 protein. Their mechanism of action is based on the destabilization of the cell division process — they prevent the formation of microtubules, which are necessary in the process of cell division.

The same mechanism of action has Taxol derivatives — one of the most commonly used antitumor agents. Based on the compounds obtained by scientists, a replacement for expensive, poorly available and highly toxic Taxol derivatives in the treatment of cancer can be created.

Article in the European Journal of Organic Chemistry.

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June 22 - 26, 2017 in Barnaul, Altai State University, took place the Summer Academy of the BRICS Youth Assembly, an international event that brought together representatives of different countries
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RUDN University organized the first 5G Summit R&D Russia on June 19 - 20, 2017
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RUDN chemist creates catalyst to produce anti-mosquito substances

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22 Oct
RUDN soil scientists developed a new method for assessing soil fertility

RUDN soil scientists have revealed a direct correlation between the rate of soil formation of carbon dioxide, called CO2 emissions, and the content of microbial biomass in it. It is known that CO2 emission from soil is mainly conditioned by respiration of soil microorganisms and plant roots. The more CO2 soil emits, the more microbial biomass it usually contains. It was shown that CO2 emission by chernozem of different ecosystems (or different types of land use) correlates with the content of microbial biomass, and most closely with the rate of its microbial respiration. And the soil with good microbial properties has the “best quality”, is more fertile, provides the highest yield of crops and other plant biomass.

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22 Oct
RUDN University chemists proposed a way to reduce three times the temperature for the oxidation of alkanes

RUDN University chemists and their colleagues from the Russian Academy of Sciences have proposed new catalysts that allow to reduce the temperature of the oxidation reaction of alkanes three times — from 150 to 50 degrees. This significantly reduces the cost of synthesizing alcohols, aldehydes and other compounds needed, in particular, for the production of nylon and capron.

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