Synthesis of a novel series of benzylether-containing  cinnamoyl derivatives as histone deacetylase  inhibitors.
Histone deacetylases (HDACs) play an important role in gene transcription, cellular proliferation, apoptosis, and tumorigenesis. A novel series of benzylether-containing cinnamoyl derivatives were designed and synthesized as inhibitors of histone deacetylases (HDACs). Most of these compounds possessed inhibitory activity against the enzymes with IC50 values as low as 30 microM. In addition, compounds 4d (IC50 = 11.1 microM) and 4n (IC50 = 7.7 microM) exhibited high antiproliferative activity against tumor cell growth and effectively induced cell cycle arrest.
Jiao
Jie
J
Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, Ji'nan, P. R. China.
Fang
Hao
H
Wang
Xuejian
X
Zhu
Huawei
H
Jiang
Lan
L
Xu
Wenfang
W
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D013329:Structure-Activity Relationship
D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases