One-Pot Gateway to Quinazoline-Thiohydantoin Fused Scaffolds and Discovery of Their Antileukemic Activity.

ABSTRACT: In drug discovery, fusing bioactive heterocyclic frameworks leads to new analogs with improved properties. Quinazoline and thiohydantoin are prominent heterocycles, recognized for their diverse pharmacological profiles. Although quinazolines fused with various heterocycles are present in numerous clinical drugs, quinazoline-thiohydantoin fused frameworks, along with their synthetic approaches, remain unreported. Here, we introduce a transition metal-free, one-pot approach that enables the efficient and high-yielding synthesis (up to 92% yield) of this previously unexplored class of heterocyclic compounds. A streamlined three-step domino reaction, enabling the formation of three C-N bonds in a single operation, followed by dehydrogenation step, results in the desired quinazoline-thio

SUBMITTER: Kersting L 

PROVIDER: S-EPMC12933347 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature