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Z-Stereoselective catalytic synthesis of natural acids, lembehynes, and acetogenins - Modern preparations for medicine
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1  Institute of Petrochemistry and Catalysis of Russian Academy of Science

Published: 31 October 2018 by MDPI in 4th International Electronic Conference on Medicinal Chemistry session ECMC-4

The report discusses the latest achievements of the authors in developing original methods for stereoselective synthesis of natural acetogenins, higher bis-methylene-separated (interrupted) di- and trienoic acids, lembehynes that are of exceptional interest as low-toxic target antitumor drugs, as well as compounds with neritogenic activity for treating neurodegenerative diseases.

The synthetic approaches to the above listed natural compounds are based on the use at the key stage of the synthesis, of new organometallic reactions, such as Ti-catalyzed homo- and cross-cyclomagnesiation of 1,2-dienes, discovered in the Laboratory of Catalytic Synthesis of the IPC RAS, involving available Grignard reagents.

The studies of the synthesized compounds for their antitumor and antibacterial activities in vitro were performed with the use of unique equipment in “Centre for Molecular Design and Biological Screening of Candidate Substances for the Pharmaceutical Industry” at the Institute of Petrochemistry and Catalysis of RAS using modern methods such as flow cytofluorometry, fluorescence microscopy and western blotting.

In silico studies into regularities of the structural influence of the synthesized compounds on their antitumor activity were fulfilled with the use of molecular docking and molecular dynamics experiments.

For compounds that showed the greatest activity, in vivo tests were performed for linear mice with grafted malignant Lewis carcinoma.

Keywords: Natural acetogenins; Higher bis-methylene-separated(interrupted) di- and trienoic acids; Lembehynes; Antitumor drugs; Neritogenic activity.