In 2016,Morera, Ludovica; Roatsch, Martin; Fuerst, Michael C. D.; Hoffmann, Inga; Senger, Johanna; Hau, Mirjam; Franz, Henriette; Schuele, Roland; Heinrich, Markus R.; Jung, Manfred published 《4-Biphenylalanine- and 3-Phenyltyrosine-Derived Hydroxamic Acids as Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A》.ChemMedChem published the findings.Formula: C4H7BrO2 The information in the text is summarized as follows:
Overexpression of the histone lysine demethylase KDM4A, which regulates H3K9 and H3K36 methylation states, has been related to the pathol. of several human cancers. We found that a previously reported hydroxamate-based histone deacetylase (HDAC) inhibitor (SW55) was also able to weakly inhibit this demethylase with an IC50 value of 25.4 μm. Herein we report the synthesis and biochem. evaluations, with two orthogonal in vitro assays, of a series of derivatives of this lead structure. With extensive chem. modifications on the lead structure, also by exploiting the versatility of the radical arylation with aryldiazonium salts, we were able to increase the potency of the derivatives against KDM4A to the low-micromolar range and, more importantly, to obtain demethylase selectivity with respect to HDACs. Cell-permeable derivatives clearly showed a demethylase-inhibition-dependent antiproliferative effect against HL-60 human promyelocytic leukemia cells. In the experiment, the researchers used Methyl 3-bromopropanoate(cas: 3395-91-3Formula: C4H7BrO2)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents.Formula: C4H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary