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Minor structural modifications to Pracinostat produce big changes in its biological responses
Author(s) -
Jia Rong,
Sun Pengju,
Zhang Yan,
Ge Youjin,
Yu Niefang
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13527
Subject(s) - chemistry , computational biology , biology
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.