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

Molecules

Seikwan Oh²  Hyung–In Moon¹  Il–Hong Son¹ 

[1]Department of Neuroscience and Inam Neuro Science Research Center, Wonkwang University Sanbon Medical Center, Sanbondong, Gunpocity, Kyunggido, 435-040, South Korea. E-mails:

[2]Department of Neuroscience and Medical Research Institute, College of Medicine, Ewha Womans University, Seoul 158–710, South Korea.

关键词: HDAC;    N–Sulfonylation;    Coupling reaction;    Anticancer;   

DOI  :  10.3390/12051125

来源: mdpi

【 摘 要 】

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.

【 授权许可】

Unknown   
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