Discovery of (Aryloxopropenyl)pyrrolyl Hydroxyamides as Selective Inhibitors of Class IIa Histone Deacetylase Homologue HD1-A
2003; American Chemical Society; Volume: 46; Issue: 23 Linguagem: Inglês
10.1021/jm034167p
ISSN1520-4804
AutoresAntonello Mai, Silvio Massa, R Pezzi, Dante Rotili, Peter Loidl, Gerald Brosch,
Tópico(s)Peptidase Inhibition and Analysis
ResumoChemical manipulations performed on aroyl pyrrolyl hydroxyamides, a new class of HDAC inhibitors previously reported by us, led to (aryloxopropenyl)pyrrolyl hydroxyamides 3a−g. Such compounds, showing better inhibitory activity against maize HD1-A than HD1-B (two homologues of mammalian class IIa and I HDACs, respectively), are the first class of IIa-selective inhibitors (fold selectivity: 7−78). They could be useful as tools for probing the biology of these enzymes and eventually as new anticancer agents with low toxicity.
Referência(s)