Synthesis and biological evaluation of vioprolide B and its dehydrobutyrine-glycine analogue.

Noé Osorio ReinekeFranziska A V ElsenHanusch A GrabDietrich Mostert Stephan A Sieber Thorsten Bach

Published in: Chemical communications (Cambridge, England) (2024)

Herein, we describe the total synthesis of the depsipeptide vioprolide B and of an analogue, in which the ( E )-dehydrobutyrine amino acid was replaced by glycine. The compounds were studied in biological assays which revealed cytotoxicity solely for vioprolide B presumably by covalent binding to cysteine residues of elongation factor eEF1A1 and of chromatin assembly factor CHAF1A.

Keyphrases

amino acid
gene expression
dna damage
transcription factor
single cell
genome wide
fluorescent probe