Chemical Synthesis of Acybolins Reveals Their Antiproliferative Activity

Abstract An efficient synthetic access to the acybolin class of inducible secondary metabolites is being reported. The approach developed features coupling between the antibiotic (−)-bactobolin A and various acybolin side chains without the need for protecting groups. The biological evaluation of synthetic acybolins in human cancer cell cultures revealed their potent antiproliferative effects.