Publication Details (including relevant citation information):
Bioorg. Med. Chem., 2010, 18 (5), 1761-1772.
Histone deacetylases (HDACs) are enzymes involved in tumor genesis and development. Herein we report a novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as HDACs inhibitors. The preliminary biological screening showed that most of our compounds exhibited potent inhibitory activity against HDACs. Within this series, five compounds, 13a (IC50=0.58±0.10 μM), 7d (IC50=1.00±0.16 μM), 8l (IC50=1.06±0.14 μM), 7i (IC50=1.17±0.19 μM) and 7a (IC50=1.29±0.15 μM) possessed better HDACs inhibitory activity than Vorinostat (IC50=1.48±0.20 μM). So these five compounds could be used as novel lead compounds for further design of HDACs inhibitors. The anti-proliferative activities of a few compounds and the structure-activity relationships are also briefly discussed.