
MOSCOW, May 29. The technology of two-stage synthesis of compounds from indoles will help to obtain components for new drugs against cancer, diabetes and malaria, NCFU scientists believe. According to them, the proposed method will simplify the production of biologically active substances valuable for medicine. The results of the study were published in the scientific journal Molecules.
Indoles are the most important class of organic molecules, the indole fragment is used in the production of many popular drugs, including those against cancer, diabetes and malaria, stressed at the North Caucasus Federal University (NCFU).
One of the suitable basic elements for the creation of biologically active substances in demand in medicine are 3-aminoindoles. They are often found in natural compounds, but they are very unstable in themselves, and the process of obtaining them in the laboratory was resource-intensive, explained Alexander Aksenov, head of the New Synthetic Methods laboratory at NCFU.
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«We have developed a new economical method for the synthesis of 3-aminoindoles. The approach is based on the reaction we studied between indoles and nitrostyrenes in the presence of phosphorous acid. We convert the resulting compound into 3-aminoindole by reacting it with hydrazine hydrate in a microwave oven,” Aksenov specified.
According to the researcher, today only a few methods for the synthesis of such molecules are known, and each of the available technologies is labor-intensive, and also involves the use of expensive and aggressive reagents. At the same time, the method of NCFU scientists is based on the use of available substances: nitrostyrene at the first stage and hydrazine or simple amino acids at the second, Aksenov added. which has pronounced antitumor and antimalarial properties. And its key fragment is precisely 3-aminoindole. Therefore, the solution of this problem is a matter of time and selection of the desired combination of components in the synthesis,» the specialist clarified.
He noted that the method is also already being used to synthesize a number of other compounds that may become especially significant for medicine. Experts send samples for bioexamination and will continue to work with the most promising ones.
The expert noted that some biologically active molecules are expected to become the basis for the development of more effective drugs against cancer, diabetes and malaria.
Also NCFU chemists continue to create an extensive library of compounds that will allow a more detailed study of the properties of molecules with indole fragments, Aksenov emphasized.
NCFU is a member of the Priority-2030 state support program for Russian universities.

