Design and Synthesis of Novel HDAC Inhibitors Based on Click Reaction
Histone deacetylase(HDAC)inhibitor is a new antitumor drug.In this paper,two active frag-ments were spliced by Click reaction to design and synthesize a new HDAC inhibitor.Compound 1 was prepared from 3-fluorophthalic anhydride by substitution reaction.Compound 4a—4c was obtained by Williamson reaction,p-toluenesulfonylation and azide reaction with 2-bromoethanol.Compound 5a—5c were obtained by Click reaction with Compound 1 and 4a—4c.The structures of the target compounds were confirmed by 1H-NMR,and the activity of the target compounds were tested by HDACs kit.The preliminary biological activity test showed that compound 5b had the same HDAC inhibitory activity as the positive control drug.
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