Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group.
Utilizing tranexamic acid as a starting material, a series of N-hydroxycarboxamides were synthesized in order to seek new histone deacetylase (HDAC) inhibitors. Further structure optimization involving the replacement of the 1,4-cyclohexylene group with the 1,4-phenylene group yielded the promising HDAC inhibitors which possess a terminal bicyclic aryl amide.
Uesato
Shinichi
S
Department of Biotechnology, Faculty of Engineering, Kansai University, Suita, 564-8680, Osaka, Japan. uesato@ipicku.kansai-u.ac.jp
Kitagawa
Manabu
M
Nagaoka
Yasuo
Y
Maeda
Taishi
T
Kuwajima
Hiroshi
H
Yamori
Takao
T
D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D003110:Colonic Neoplasms; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000577:Amides; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors