Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA |
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| Authors: | Hanessian Stephen Vinci Valerio Auzzas Luciana Marzi Mauro Giannini Giuseppe |
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| Institution: | Department of Chemistry, Université de Montréal, PO Box 6128, Station Centre-ville, Montréal, Que., Canada H3C 3J7. stephen.hanessian@umontreal.ca |
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| 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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