N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.

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Giannini G, Marzi M, Pezzi R, Brunetti T, Battistuzzi G, Marzo MD, Cabri W, Vesci L, Pisano C

N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. doi: 10.1016/j.bmcl.2009.02.029. Epub 2009 Feb 12.

PubMed ID

19285395 [ View in PubMed

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Abstract

With the aim to discover novel HDAC inhibitors with high potency and good safety profiles, we have designed a small library based on a N-hydroxy-(4-oxime)-cinnamide scaffold. We describe the synthesis of these novel compounds and some preliminary in vitro cytotoxic activity on three tumor cell lines, NB4, H460 and HCT116, as well as their inhibitory activity against class I, II and IV HDAC. Several 4-oxime derivatives demonstrated a promising inhibitory activity on HDAC6 and HDAC8 coupled to a good selectivity profile.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Trichostatin A	Histone deacetylase 7	IC 50 (nM)	22	N/A	N/A	Details