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Updated: Jun 19, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Azetidinones as zinc-binding groups to design selective HDAC8 inhibitors
Paola Galletti1, Arianna Quintavalla, Caterina Ventrici
1Dipartimento di Chimica G. Ciamician, Università of Bologna, Via Selmi 2, 40126 Bologna, Italy.
Abstract:
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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