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Synthesis and biological activity of [Tic5] didemnin B
A J Pfizenmayer1, M D Vera, X Ding
1Department of Chemistry, University of Pennsylvania, Philadelphia 19104-6323, USA.
Bioorganic & Medicinal Chemistry Letters
|February 6, 1999
Abstract:
A didemnin B analog containing a Tic (1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) as a conformationally restrained replacement for tyrosine has been synthesized and shown to have comparable potency as a protein biosynthesis inhibitor. Synthetic highlights include an oxidation of an alcohol to an acid in the presence of the sensitive Tic heterocycle and a modified Schmidt-type one-pot macrocyclization.