期刊
CHEMMEDCHEM
卷 4, 期 12, 页码 1991-2001出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.200900309
关键词
azetidinones; heterocycles; histone deacetylase; inhibitors; lactams
2-Azetidinones, commonly known as beta-lactams, are well-known heterocyclic compounds. Herein we described the synthesis and biological evaluation of a series of novel beta-lactams. In vitro inhibition assays against HDAC isoforms showed an interesting isoform-selectivity of these compounds towards HDAC6 and HDAC8. The isoform selectivity changed in response to modification of the azetidinone-ring nitrogen atom substituent. The presence of an N-thiomethyl group is a prerequisite for the activity of these compounds in the micromolar range towards HDAC8.
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