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

Title
Synthesis of sulfonamides and evaluation of their histone deacetylase (HDAC) activity
Authors
Oh S.Moon H.-I.Son I.-H.Jung J.-C.
Ewha Authors
오세관정재철
SCOPUS Author ID
오세관scopus
Issue Date
2007
Journal Title
Molecules
ISSN
1420-3049JCR Link
Citation
vol. 12, no. 5, pp. 1125 - 1135
Indexed
SCIE; SCOPUS WOS scopus
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.
DOI
10.3390/12051125
Appears in Collections:
의과대학 > 의학과 > Journal papers
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