HPLC of Formula: 3395-91-3In 2017 ,《Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors》 was published in ACS Medicinal Chemistry Letters. The article was written by Taha, Taha Y.; Aboukhatwa, Shaimaa M.; Knopp, Rachel C.; Ikegaki, Naohiko; Abdelkarim, Hazem; Neerasa, Jayaprakash; Lu, Yunlong; Neelarapu, Raghupathi; Hanigan, Thomas W.; Thatcher, Gregory R. J.; Petukhov, Pavel A.. The article contains the following contents:
Histone deacetylase 8 (HDAC8) is a promising drug target for multiple therapeutic applications. Here, we describe the modeling, design, synthesis, and biol. evaluation of a novel series of C1-substituted tetrahydroisoquinoline (TIQ)-based HDAC8 inhibitors. Minimization of entropic loss upon ligand binding and use of the unique HDAC8 “”open”” conformation of the binding site yielded a successful strategy for improvement of both HDAC8 potency and selectivity. The TIQ-based I and II exhibited the highest 82 and 55 nM HDAC8 potency and 330- and 135-fold selectivity over HDAC1, resp. Selectivity over other class I isoforms was comparable or better, whereas inhibition of HDAC6, a class II HDAC isoform, was below 50% at 10 μM. The cytotoxicity of I and II was evaluated in neuroblastoma cell lines, and II displayed concentration-dependent cytotoxicity similar to or better than that of PCI-34051. The selectivity of I and II was confirmed in SH-SY5Y cells as both did not increase the acetylation of histone H3 and α-tubulin. Discovery of the novel TIQ chemotype paves the way for the development of HDAC8 selective inhibitors for therapeutic applications. In the part of experimental materials, we found many familiar compounds, such as Methyl 3-bromopropanoate(cas: 3395-91-3HPLC of Formula: 3395-91-3)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.HPLC of Formula: 3395-91-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary