Exploring chemical substructures essential for hERG K(+) Channel blockade by synthesis and biological evaluation of dofetilide analogues

Abstract

We designed and synthesized 40 analogues of dofetilide and established structure-activity relationships for their interaction with hERG potassium channel. The data were derived with the aim to specify structural features that give rise to hERG toxicity.

Keywords

• cardiotoxicity
• dofetilide
• hERG
• ion channels
• radioligand binding assays
• structure-activity relationships