Tuesday, October 15, 2024

New electrophiles targeting thiols in a reversible covalent manner

Xingyu Ma,   Manyi Xu,   Fengge Wang,  Tingting Hu,  Xinyuan Chena  and  Chong-Jing Zhang

Chem. Commun., 2024
DOI
https://doi.org/10.1039/D4CC04612A

Reversible covalent electrophiles with the advantages of both reversible and covalent interactions receive much attention in the fields of chemical biology and medicinal chemistry. Here, we report two electron-deficient olefins activated by amide and ester, amide-substituted acrylamide and methyl ester-substituted acrylamide, targeting thiols in a reversible covalent manner.

Covalent Probes Reveal Small-Molecule Binding Pockets in Structured RNA and Enable Bioactive Compound Design

Sandra Kovachka, Jielei Wang, Amirhossein Taghavi, Yilin Jia, Taro Asaba, Karen C. Wolff, Mason Martin, Xueyi Yang, Samantha M. Meyer, Sabin...