History
The chemistry of steroids as a direction of research in the USSR was initiated by Acad. I.N. Nazarov in the late 50s. Initially, 3 groups were organized - I.V. Trade, L.D. Bergelson (both later became members of the Institute of Chemistry of Natural Compounds of the USSR Academy of Sciences) and the group of chemistry of corticoid compounds A.A. Akhrem, which on October 9, 1962 was transformed into the Laboratory of Chemistry of Corticoid Compounds. 1973 to 2009 the laboratory was headed by D.Sc. A.V. Kamernitsky. From 2009 to the present, the head of the laboratory is Doctor of Chemical Sciences. I.V. Zavarzin. During its existence, the range of research of the laboratory has expanded significantly, so in 2010 it was named “Laboratory of the chemistry of steroid compounds”. Today Medicinal chemistry We apply the developed methodology for concise synthesis of medically relevant steroidal compounds. The research is supported by computational chemistry methods, such as molecular docking, and evaluation of biological activity in vitro and in vivo. New synthetic methods Our group has a longstanding interest in developing the synthetic methodology based on the multifunctional reagents reactivity. Our key advances in this area are related to the exploration of the synthetic value of oxamic acids thiohydrazides and their analogs. We extensively use high-tech equipment, including high pressure devises and continuous flow reactors.
The most successful line of research has been the creation and modification of pentacyclic steroid derivatives. The discovery was made in the laboratory that 16-dehydropregnenolone acetate is capable of acting as a dienophile in the Diels-Alder reaction with 1,3-dienes. This led to the creation of a new class of progesterone analogs, a detailed study of their structure, chemical and biological properties in vivo and in vitro. On the basis of the most promising pentarans, two original hormonal drugs were created: the combined contraceptive drug Metzigepron and then the therapeutic drug Metzigeston for the treatment of progesterone-deficient conditions in women. In vivo metabolism was studied and innovative dosage forms with increased bioavailability were created. In recent years, the Laboratory has developed original approaches to the synthesis of various types of steroids containing heterocyclic fragments. The direction associated with the production and modification of secosteroids is also successfully developing. This has resulted in a number of potential anticancer agents that are currently being tested.
These works were highly appreciated: in 2004 the head of the laboratory, D.Sc. A.V. Kamernytsky and Leading Scientific Researcher, Doctor of Chemical Sciences I.S. Levin were awarded the Academic Prize. M.M. Shemyakin.
In recent years, the Laboratory has developed original approaches to the synthesis of various types of steroids containing heterocyclic fragments. The direction associated with the production and modification of secosteroids is also successfully developing. This has resulted in a number of potential anticancer agents that are currently being tested.
Today
