Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 25, Issue 1, Pages 30-39Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-015-1446-1
Keywords
Fatty acids; Cyclomagnesiation; Homogeneous catalysis; Topoisomerase I and II alpha inhibitors; Docking; Stereoselective synthesis of nZ,(n+4) Z-dienoic acids
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Funding
- Russian Science Foundation [14-13-00263]
- Russian Science Foundation [14-13-00263] Funding Source: Russian Science Foundation
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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.
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