Synthesis of sulfonamides and evaluation of their histone deacetylase (HDAC) activity.
نویسندگان
چکیده
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 microM in vitro.
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ورودعنوان ژورنال:
- Molecules
دوره 12 5 شماره
صفحات -
تاریخ انتشار 2007