Preparation method of rubiaceous cyclopeptide and application of rubiaceous cyclopeptide as Hippo-YAP signal pathway inhibitor

2014 
The invention provides an application of rubiaceous cyclopeptide RA-V (1) as a Hippo-YAP signal pathway inhibitor, a preparation method of the rubiaceous cyclopeptide and an application of the rubiaceous cyclopeptide to preparation of drugs for treating and preventing YAP abnormal activation related cancers. The rubiaceous cyclopeptide provided by the invention is formed by condensation of peptide bonds of one alpha-D-alanine, one alpha-L-alanine, three substituted N-methyl-alpha-L-tyrosine and one alpha-L-amino acid of other types, and six amino acids are condensed to form an eighteen-membered ring, wherein a benzene ring between two vicinal tyrosines is connected through an oxygen bridge to form a fourteen-membered ring. Compared with the prior art, the preparation method provided by the invention can be used for rapidly separating and purifying the target compound RA-V (1) and has the advantages of high efficiency, strong purposiveness, few separation step, convenience in operation, good controllability and repeatability, recyclable solvent, low cost and suitability for industrial production.
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