Synthesis of steroids containing the azole fragment in the cycle D and/or in the side chain as the basis for creating medicines for the treatment of prostate cancer


Bilateral project with Republic of Belarus

Strategic priority

I. Health

Strategic direction

3. Pharmaceuticals and nutraceuticals



The project is focused on the design and practical development of the new biopharmaceutical agents belonging to the class of steroids, to be involved in the treatment of prostate cancer. The idea of ​​the project is based on the results of international research described in recent years, including the achievements obtained at Institute of Bioorganic Chemistry of National Academy of Sciences of Belarus on the synthesis and study of the activity of steroid antiandrogens, as well as Institute of Chemistry in the field of synthesis of heterocycles. It consists of the development of methods for the synthesis of the nitrogen-containing heterocyclic fragment in the side chain and/or in the D cycle of the new steroid molecules that meet the following requirements for the structure of CYP17A1 inhibitors: 1) the presence of a nitrogen-containing substituent in the cycle D and/or in the side chain, in which the lone pair of electrons is localized on the N atom; 2) sp2- or sp3- hybridization of the C(17) atom; 3) a suitable spatial orientation of groups capable of forming hydrogen bonds with CYP17A1 (3β-hydroxyl group and an N in cycle D and/or in the side chain; 4) the presence of hydrophobic substituents from the β-side of the steroid fragment, and which will be endowed with a complex of beneficial therapeutic properties and differ from the existing drugs by the lower toxicity and higher efficiency. New methodical approaches and products of synthesis created in the frame of the project, as well as the data of biological screening of the obtained new substances, and conclusions about the prospects and paths of implementation, will constitute a scientific and technological basis for the further development of the work in this area and promoting their results into clinical practice.