Synthesis of sulfonamides and evaluation of their histone deacetylase (HDAC) activity

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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 μM in vitro. © 2007 by MDPI.

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Oh, S., Moon, H. I., Son, I. H., & Jung, J. C. (2007). Synthesis of sulfonamides and evaluation of their histone deacetylase (HDAC) activity. Molecules, 12(5), 1125–1135. https://doi.org/10.3390/12051125

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