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RUDN chemist, along with colleagues from the RAS Institutes, simplified the synthesis of antitumor compounds

RUDN chemist, along with colleagues from the RAS Institutes, simplified the synthesis of antitumor compounds

A RUDN chemist in collaboration with colleagues from N.D. Zelinsky Institute of Organic Chemistry and N.K. Koltsov Institute of Developmental Biology (IDB), RAS have developed a new method for the synthesis of isoxazole derivatives — substances that destabilize the process of cell division and potentially may become the basis for new anti-cancer drugs. The new method is based on the use of easily available reagents and does not require high temperatures.

Many modern anticancer drugs are toxic, difficult to access and/or very expensive. Moreover, tumor cells may develop resistance to the drugs used. Therefore, researchers study the biological properties of molecules in order to obtain new antitumor drugs with optimal properties. One of the common approaches to the search for such drugs is testing of analogues of substances that already showed antitumor activity. Such substances include, in particular, isoxazole derivatives that inhibit — “turn off” — the Hsp90 protein, which is necessary for the survival of tumor cells. However, compounds of this class are inaccessible due to the complexity of the synthesis procedure, which requires, in particular, the complete absence of water molecules, and the reagents are expensive and toxic.

RUDN chemist Viktor Khrustalev and his colleagues developed a method for the synthesis of isomers of these substances, that is, the compounds that are identical in atomic composition but different in the arrangement of atoms in space. Easily accessible derivatives of arylnitromethanes and chloroacetamides were used as raw materials, and the reaction itself was carried out at temperatures not exceeding 80 degrees at atmospheric pressure and did not require anhydrous conditions.

The obtained substances had anticancer activity, but unlike the prototype compounds, they did not inhibit Hsp90 protein. Their mechanism of action is based on the destabilization of the cell division process as they prevent the formation of microtubules, which are important in the process of cell division.

Taxol derivatives, one of the most commonly used antitumor agents, have the same mechanism of action. Basing on the compounds obtained by the scientists, it is possible to create a substitute for an expensive, inaccessible and highly toxic derivatives of taxol in the treatment of cancer.

The work was published in European Journal of Organic Chemistry. 

International scientific cooperation View all
03 Nov 2017
The main goal of the RUDN University and UNISDR Office for Northeast Asia and Global Education and Training Institute for Disaster Risk Reduction at Incheon (UNISDR ONEA-GETI) cooperation is to obtain knowledge about disaster risk reduction and international experience in this area for creating training courses for basic and additional professional education in RUDN
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03 Nov 2017
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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30 Dec
Biologists from RUDN University discovered the secret of flaxseed oil with long shelf life

Biologists from RUDN University working together with their colleagues from the Institute of Molecular Biology of the Russian Academy of Sciences and the Institute of Flax studied the genes that determine the fatty acid composition in flaxseed oil and identified polymorphisms in six of them. The team also found out what gene variations could extend the shelf life of flaxseed oil. This data can be used to improve the genetic selection of new flax breeds. The results were published in the BMC Plant Biology journal.

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11 Oct
Mowing Is More Harmful to Soil Than Grazing

A team of biologists analyzed soil samples from a pasture and a regularly mowed meadow and found out that grazing lets more carbon get into the soil than mowing. This, in turn, improves the carbon cycle and makes microorganisms more efficient.

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11 Oct
Soil scientists suggest method for remediating urban garden soils contaminated with lead and arsenic

The soils of urban gardens and vegetable patches contain a lot of toxicants (including lead and arsenic) in high concentrations which can be harmful to the health of children and people with chronic diseases. A team of soil scientists from RUDN University suggested a remediation method developed based on data collected in a garden of Brooklyn (NY, U.S.).

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