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

Salvatore Di Maro, Rey Chen Pong, Jer Tsong Hsieh, Jung Mo Ahn

Research output: Contribution to journalArticle

25 Citations (Scopus)

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 compounds.

Original languageEnglish (US)
Pages (from-to)6639-6641
Number of pages3
JournalJournal of Medicinal Chemistry
Volume51
Issue number21
DOIs
StatePublished - Nov 13 2008

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Solid-Phase Synthesis Techniques
Histone Deacetylase Inhibitors
Acids
romidepsin
Neoplasms

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Efficient solid-phase synthesis of FK228 analogues as potent antitumoral agents. / Di Maro, Salvatore; Pong, Rey Chen; Hsieh, Jer Tsong; Ahn, Jung Mo.

In: Journal of Medicinal Chemistry, Vol. 51, No. 21, 13.11.2008, p. 6639-6641.

Research output: Contribution to journalArticle

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