Lin, Xianfeng published the artcileDesign and Synthesis of Orally Bioavailable Aminopyrrolidinone Histone Deacetylase 6 Inhibitors, Recommanded Product: Methyl 4-bromo-3-chlorobenzoate, the publication is Journal of Medicinal Chemistry (2015), 58(6), 2809-2820, database is CAplus and MEDLINE.
Histone deacetylase 6 (HDAC6) removes the acetyl group from lysine residues in a number of non-histone substrates and plays important roles in microtubule dynamics and chaperone activities. There is growing interest in identifying HDAC6-selective inhibitors as chem. biol. tools and ultimately as new therapeutic agents. Herein we report the design, synthesis, and phenotypic screening of a novel class of 3-aminopyrrolidinone-based hydroxamic acids as HDAC6 inhibitors. In particular, the α-methyl-substituted enantiomer I (3-S) showed significant in-cell tubulin acetylation (Tub-Ac) with an EC50 of 0.30 μM but limited impact on p21 levels at various concentrations In enzyme inhibition assays, I demonstrated high selectivity for HDAC6 with an IC50 of 0.017 μM and selectivity indexes of 10 against HDAC8 and over 4000 against HDAC1-3 isoforms. Moreover, I has suitable drug metabolism and pharmacokinetics properties compared with other hydroxamic acid-based HDAC inhibitors, warranting further biol. studies and development as a selective HDAC6 inhibitor.
Journal of Medicinal Chemistry published new progress about 117738-74-6. 117738-74-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Ester, name is Methyl 4-bromo-3-chlorobenzoate, and the molecular formula is C8H6BrClO2, Recommanded Product: Methyl 4-bromo-3-chlorobenzoate.
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