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

Seikwan Oh, Hyung In Moon, Il Hong Son, Jae Chul Jung

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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.

Original languageEnglish
Pages (from-to)1125-1135
Number of pages11
JournalMolecules
Volume12
Issue number5
DOIs
StatePublished - May 2007

Keywords

  • Anticancer
  • Coupling reaction
  • HDAC
  • N-sulfonylation

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