Literature DB >> 16870438

Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA.

Stephen Hanessian1, Valerio Vinci, Luciana Auzzas, Mauro Marzi, Giuseppe Giannini.   

Abstract

Analogues of suberoylanilide hydroxamic acid (SAHA) were prepared by replacing the Zn-binding group with squaric acid, N-hydroxyurea, and 4-hydroxymethyl oxazoline units, also varying the length of the aliphatic chain. No inhibitory activity on HDAC was observed below 1.0 microM and no cytotoxic activity on different tumor cell lines was seen below 20.0 microM.

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Year:  2006        PMID： 16870438     DOI： 10.1016/j.bmcl.2006.06.090

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

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Authors:  William Doherty; Eva-Maria Dürr; Hannah T Baddock; Sook Y Lee; Peter J McHugh; Tom Brown; Mathias O Senge; Eoin M Scanlan; Joanna F McGouran
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