Biomass Conversion to High Value Chemicals: From Furfural to Chiral Hydrofuroins in Two Steps

Catalytic asymmetric transfer hydrogenation of <i>rac</i>-furoin and furil produces hydrofuroin with up to 99% <i>ee</i> and 9:1 <i>dr</i>. This reaction provides an exceptionally easy access to optically active hydrofuroins in two straightforward steps from biomass-derived furfural (global production 200 000–300 000 t annually) using benzoin condensation

Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity

International audienceDNA-methyltransferases (DNMTs) are a class of epigenetic enzymes that catalyze the transfer of a methyl moiety from the methyl donor S-adenosyl-L-methionine onto the C5 position of cytosine in DNA. This process is dysregulated in cancers and leads to the hypermethylation and silencing of tumor suppressor genes. The development of potent and selective inhibitors of DNMTs is of utmost importance for the discovery of new therapies for the treatment of cancer. We report herein the synthesis and DNMT inhibitory activity of 29 analogues derived from NSC 319745. The effect of selected compounds on the methylation level in the MDA-MB-231 human breast cancer cell line was evaluated using a luminometric methylation assay. Molecular docking studies have been conducted to propose a binding mode for this serie