Novel structural analogues of a HDAC inhibitor FK228 have been synthesized by modifying the most synthetically challenging unit, (3S,4E)-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 compound.

Efficient Solid-Phase Synthesis of FK228 Analogues as Potent Antitumoral Agents

DI MARO, Salvatore;
2008

Abstract

Novel structural analogues of a HDAC inhibitor FK228 have been synthesized by modifying the most synthetically challenging unit, (3S,4E)-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 compound.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11591/385804
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