Minor structural modifications to Pracinostat produce big changes in its biological responses
A series of compounds similar to Pracinostat that contained benzimidazole ring and N-hydroxyacrylamide attached at 5- or 6-position were designed, synthesized, and evaluated as HDAC inhibitors. It was interesting to find that the corresponding derivative 1 with N-hydroxyacrylamide attached at 5-position was a potent HDAC inhibitor while the others at 6-position were not. This is the first time to demonstrate the position difference plays important role in the HDAC inhibitory activities of the cinnamic hydroxamates.
THE SYNTHESIS OF 3-CHLORO-4-NITRO- AND 4-AMINO-3-CHLORO-BENZYL ALCOHOLS
The synthesis of the new compounds 3-chloro-4-nitro- and 4-amino-3-chloro-benzyl alcohols is described.Nitration of 3-chloro-benzyl chloride gives two isomers; the 3-chloro-4-nitrobenzyl chloride isomer is converted to the alcohol via an ester intermediat
Silk, Nicholas A.,Martin, Carl N.
p. 2133 - 2139
(2007/10/02)
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