NZ,(N + 4)Z-DIENOIC FATTY ACIDS: A NEW METHOD FOR THE SYNTHESIS AND INHIBITORY ACTION ON TOPOISOMERASE I AND IIA

Abstract:

An original, effective approach to the stereoselective method for the synthesis of higher unsaturated acids containing a 1Z,5Z-diene group in 61–75 % yields and with >98 % selectivity based on the new intermolecular Cp2TiCl2-catalyzed cross-cyclomagnesiation of terminal aliphatic and O-containing 1,2-diene with Grignard reagents has been developed. The inhibitory action of the obtained dienoic acids on the human topoisomerase I and II was studied. Resorting to the data of molecular docking, a probable mechanism of inhibition was proposed.

Тип: Article