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• Moon, H
• Son, I
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• Son, I
• Jung, J
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• Moon, H
• Son, I
• Jung, J

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Molecules 2007, 12(5), 1125-1135; doi:10.3390/12051125

Article

Synthesis of Sulfonamides and Evaluation of Their Histone Deacetylase (HDAC) Activity

Seikwan Oh¹ , Hyung–In Moon² , Il–Hong Son²  and Jae–Chul Jung^1,*

¹ Department of Neuroscience and Medical Research Institute, College of Medicine, Ewha Womans University, Seoul 158–710, South Korea ² Department of Neuroscience and Inam Neuro Science Research Center, Wonkwang University Sanbon Medical Center, Sanbondong, Gunpocity, Kyunggido, 435-040, South Korea

* Author to whom correspondence should be addressed.

Received: 17 April 2007; in revised form: 18 May 2007 / Accepted: 18 May 2007 / Published: 24 May 2007

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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.

Keywords: HDAC; N–Sulfonylation; Coupling reaction; Anticancer

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