Document Report Card

ID: ALA1142513

Journal: J Med Chem

Title: Efficient solid-phase synthesis of FK228 analogues as potent antitumoral agents.

Authors: Di Maro S, Pong RC, Hsieh JT, Ahn JM.

Abstract: Novel structural analogues of a HDAC inhibitor FK228 have been synthesized by modifying the most synthetically challenging unit, (3 S,4 E)-3-hydroxy-7-mercaptoheptenoic acid, with simple isosteric substitutions. These changes did not alter the backbone structure from FK228 but enabled facile and rapid synthesis by using readily available starting materials and high-yielding reactions. FK228 analogues were examined for their antitumoral activity on a variety of human cancer cells and led to the identification of new potent compounds.

CiteXplore: 18839938

DOI: 10.1021/jm800959f