Lobachevsky University scientists develop a new method for synthesizing compounds to enhance the activity of antitumour drugs

Scientists from the UNN Department of Organic Chemistry have developed a method to introduce multiple aminomethyl groups into biologically active compounds that inhibit the growth of cancer cells. This technology has the potential to enhance the effectiveness of existing anticancer drugs. With a product yield of 90% and a purity exceeding 95%, the method shows promise for application in the pharmaceutical industry.

"The biological activity of the compounds we synthesized was extensively studied in the 1980s. However, due to their specific chemical structure, these compounds were unstable and prone to rapid degradation, which complicated their practical use. We employed zinc chloride as a catalyst to prevent the molecule from breaking down during the synthesis process. Considering the high yield and purity of the product, this reaction will be of interest to both researchers and the pharmaceutical industry,"explained Vasily Otvagin, the author of the study and an associate professor at the UNN Department of Organic Chemistry.

Aminomethyl groups can act as pharmacophore fragments that enhance the effectiveness of anticancer drugs. As part of complex biologically active molecules, they enhance their effectiveness. The reaction developed by researchers from Nizhny Novgorod makes it possible to introduce such novel fragments into existing pharmaceutical formulations.

"Currently, using our method, we are synthesizing other biologically active compounds, including those that were previously unknown. For instance, we produce substances with complex nitrogen-containing heterocycles that may potentially exhibit significant biological activity. The reaction also enables single-step binding of peptides targeting tumour cells," shared Ekaterina Kudryashova, a junior researcher at the UNN Department of Organic Chemistry

The research involved scientists from the Department of Organic Chemistry at the Faculty of Chemistry, the Research Institute of Chemistry, and the Department of Biophysics at the Institute of Biology and Biomedicine of Lobachevsky University, in collaboration with the A.N. Nesmeyanov Institute of Organoelement Compounds of the Russian Academy of Sciences. The study was conducted as part of the Russian Science Foundation project "Developing effective methods for synthesizing pharmacophore groups based on available iminium electrophiles."

The findings have been published in the international journal Organic Chemistry Frontiers.