RUDN chemist, along with colleagues from the RAS Institutes, simplified the synthesis of antitumor compounds
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.
RUDN University physicians have identified genetic characteristics that may affect the predisposition to re-stenosis — narrowing of the lumen of the vessel — after the installation of a stent. The results will help to determine the risk of restenosis and select personalized therapy more accurately.
RUDN chemists have created a reusable catalyst for the oxidation of sulfides for the synthesis of drugs, dyes, and other compounds. It can “switch” the final product and provides “green” reaction conditions.
RUDN University and Shahid Beheshti University (SBU) chemist together with colleagues from Iran created a hydrogel film for wound dressing. It protects the wound from germs and is harmless to healthy tissues. Moreover, its porous structure can hold antibiotic, which kills dangerous microorganisms and provide additional protection.
RUDN University physicians have identified genetic characteristics that may affect the predisposition to re-stenosis — narrowing of the lumen of the vessel — after the installation of a stent. The results will help to determine the risk of restenosis and select personalized therapy more accurately.
RUDN chemists have created a reusable catalyst for the oxidation of sulfides for the synthesis of drugs, dyes, and other compounds. It can “switch” the final product and provides “green” reaction conditions.
RUDN University and Shahid Beheshti University (SBU) chemist together with colleagues from Iran created a hydrogel film for wound dressing. It protects the wound from germs and is harmless to healthy tissues. Moreover, its porous structure can hold antibiotic, which kills dangerous microorganisms and provide additional protection.