Totally synthetic analogues of siastatin B: III - Trifluoroacetamide analogues having inhibitory activity for tumor metastasis

Article abstract of DOI:10.7164/antibiotics.47.101

A trifluoroacetamide analogue of siastatin B, (35,45,5R,6R)-6-(trifluoroacetamido)-4,5-dihydroxy-3- piperidinecarboxylic acid has been chemically synthesized. This compound, as well as the previously synthesized analogue, (3R,4R,5R,6R)-6-(trifluoroacetamido)-3,4,5- trihydroxy-3-piperidinecarboxylic acid, showed marked inhibitory activity against β-glucuronidase and significant inhibition of experimental pulmonary metastasis of the highly metastatic melanoma B16.