2
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.

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
808
Scientific Conferences View all
03 Nov 2017
RUDN University organized the first 5G Summit R&D Russia on June 19 - 20, 2017
1147
Similar newsletter View all
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.

258
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.

16
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.).

18
Similar newsletter View all