Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors

Add time:07/14/2019    Source:sciencedirect.com

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.

We also recommend Trading Suppliers and Manufacturers of D-7-hydroxy-6,8-diiodo-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (cas 160080-87-5). Pls Click Website Link as below: cas 160080-87-5 suppliers

Prev:Discovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability
Next:Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents)