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N-Hydroxy-(4-oxime)-cinnamide: A versatile scaffold for the synthesis of novel histone deacetilase (HDAC) inhibitors

2009; Elsevier BV; Volume: 19; Issue: 8 Linguagem: Inglês

10.1016/j.bmcl.2009.02.029

1464-3405

Giuseppe Giannini, Mauro Marzi, R Pezzi, Tiziana Brunetti, Gianfranco Battistuzzi, Maria Di Marzo, Walter Cabri, Loredana Vesci, Claudio Pisano,

Click Chemistry and Applications

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.