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

✍ Scribed by Erinprit K. Singh; Lidia A. Nazarova; Stephanie A. Lapera; Leslie D. Alexander; Shelli R. McAlpine

Publisher: Elsevier Science
Year: 2010
Tongue: French
Weight: 667 KB
Volume: 51
Category: Article
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2010.06.050

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✦ Synopsis

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.

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