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.

30 Jan 2018
The conference on international arbitration, where law students from European universities simulate court proceedings and alternately defend the interests of the respondent and the orator.
821
International Projects View all
Similar newsletter View all
31 Mar
RUDN University awards for specific areas of science and technology based on the results of 2021

Every year, RUDN University selects the best of the best in the field of science and innovation and encourages with a special reward. Since 2009, the Academic Council of the University has been awarding one reward in natural and technical sciences and the other one in social and humanitarian sciences. Both individual researchers and groups of authors can become laureates.

72
31 Mar
International Day of Women and Girls in Science: women scientists of the RUDN talk about their path to science

“Science is the basis of all progress that facilitates the life of mankind and reduces its suffering,” — Marie Sklodowska—Curie. A symbol of a woman’s success in science. The first scientist in the world — twice winner of the Nobel Prize.

314
31 Mar
RUDN University Mathematicians Create a Model for Queue Organizing with Self-Sustained Servers

RUDN University mathematicians proposed a model for optimizing the operation of queuing systems (from computer networks to stores). Unlike analogues, the servers in it are self-sustained. They can determine when to start and stop working themselves. Such a model can be useful, for example, for online taxi services and other systems where workers choose their own operating hours.

80
Similar newsletter View all