<i>N</i>-Arylsulfonamide-based adenosine analogues to target RNA cap <i>N</i>7-methyltransferase nsp14 of SARS-CoV-2
Rostom Ahmed‐Belkacem, Joris Troussier, Adrien Delpal, Bruno Canard, Jean‐Jacques Vasseur, Étienne Decroly, Françoise Debart
Abstract
SAH-derived bisubstrates of SARS-CoV-2 cap RNA N 7-methyltransferase were synthesized, and two adenosines with an N -arylsulfonamide core attached by an N -ethylthioether linker proved to be effective inhibitors in the submicromolar range.
Topics & Concepts
MethyltransferaseRNALinkerChemistryAdenosineStereochemistryBiochemistryMolecular biologyBiologyComputer scienceDNAGeneMethylationOperating systemRNA and protein synthesis mechanismsRNA modifications and cancerDNA and Nucleic Acid Chemistry