Histone deacetylase inhibitors: synthesis of cyclic tetrapeptides and their triazole analogs

Histone deacetylase inhibitors: synthesis of cyclic tetrapeptides and their triazole analogs

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

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Bibliographic Details
Published in:Tetrahedron letters Vol. 51; no. 33; pp. 4357 - 4360
Main Authors: Singh, Erinprit K., Nazarova, Lidia A., Lapera, Stephanie A., Alexander, Leslie D., McAlpine, Shelli R.
Format: Journal Article
Language:English
Published: England Elsevier Ltd 18-08-2010
Online Access:Get full text
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Description
Summary:Synthesis of nine macrocyclic peptide HDAC inhibitors and three triazole derivatives is described. HDAC inhibitory activity of these compounds against HeLa cell lysate is evaluated. The biological data demonstrate that incorporation of a triazole unit improves the HDAC inhibitory activity.
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ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2010.06.050