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Histone Deacetylase Inhibitors: Synthesis of Cyclic Tetrapeptides and their Triazole Analogues.

ABSTRACT: Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives are described. HDAC inhibitory activity of these compounds against HeLa cell lysate is evaluated. The biological data demonstrates that incorporation of a triazole unit improves the HDAC inhibitory activity.

SUBMITTER: Singh EK

PROVIDER: S-EPMC2941989 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature

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Histone Deacetylase Inhibitors: Synthesis of Cyclic Tetrapeptides and their Triazole Analogues.

Singh Erinprit K EK Nazarova Lidia A LA Lapera Stephanie A SA Alexander Leslie D LD McAlpine Shelli R SR

Tetrahedron letters 20100801 33

Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives are described. HDAC inhibitory activity of these compounds against HeLa cell lysate is evaluated. The biological data demonstrates that incorporation of a triazole unit improves the HDAC inhibitory activity. ...[more]

PMID: 20865132

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