Suzuki, Takayoshi published the artcileRapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries, Application In Synthesis of 1997-80-4, the publication is Journal of Medicinal Chemistry (2012), 55(22), 9562-9575, database is CAplus and MEDLINE.
To find HDAC8-selective inhibitors, we designed a library of HDAC inhibitor candidates, each containing a zinc-binding group that coordinates with the active-site zinc ion, linked via a triazole moiety to a capping structure that interacts with residues on the rim of the active site. These compounds were synthesized by using click chem. Screening identified HDAC8-selective inhibitors including (I) (IC50 = 0.070 μM), which was more potent than PCI-34058 (IC50 = 0.31 μM), a known HDAC8 inhibitor. Mol. modeling suggested that the phenylthiomethyl group of I binds to a unique hydrophobic pocket of HDAC8, and the orientation of the phenylthiomethyl and hydroxamate moieties (fixed by the triazole moiety) is important for the potency and selectivity. The inhibitors caused selective acetylation of cohesin in cells and exerted growth-inhibitory effects on T-cell lymphoma and neuroblastoma cells (GI50 = 3-80 μM). These findings suggest that HDAC8-selective inhibitors have potential as anticancer agents.
Journal of Medicinal Chemistry published new progress about 1997-80-4. 1997-80-4 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,Benzene, name is 1-(2-Bromoethyl)-3-(trifluoromethyl)benzene, and the molecular formula is C9H9BrO2, Application In Synthesis of 1997-80-4.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary