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Updated: Jul 11, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Synthesis of sulfonamides and evaluation of their histone deacetylase (HDAC) activity
Seikwan Oh1, Hyung-In Moon, Il-Hong Son
1Department of Neuroscience and Medical Research Institute, College of Medicine, Ewha Womans University, Seoul 158-710, South Korea.
Abstract:
A simple synthesis of sulfonamides 4-22 as novel histone deacetylase (HDAC) inhibitors is described. The key synthetic strategies involve N-sulfonylation of L-proline benzyl ester hydrochloride (2) and coupling reaction of N-sulfonyl chloride 3 with amines in high yields. It was found that several compounds showed good cellular potency with the most potent compound 20 exhibiting an IC50 = 2.8 microM in vitro.
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