Visible Light-Promoted Divergent Benzoheterocyclization from Aldehydes for DNA-Encoded Chemical Libraries
Xianfu Fang, Yiting Wang, Pengyang He, Huilin Liao, Gong Zhang, Yangfeng Li, Yizhou Li
Abstract
Benzoheterocyclics have been widely adopted as drug-like core scaffolds that can be incorporated into DNA-encoded chemical library technology for high-throughput hit discovery. Here, we present a visible light-promoted divergent synthesis of on-DNA benzoheterocycles from aldehydes. Four types of DNA-conjugated benzoheterocyclics were obtained under mild conditions with a broad substrate scope. A cross substrate scope study, together with enzymatic ligation and subsequent chemical diversifications, were conducted, demonstrating the feasibility of this approach in DNA-encoded chemical library construction.
Topics & Concepts
ChemistryDNASubstrate (aquarium)Conjugated systemCombinatorial chemistryScope (computer science)Drug discoveryChemical biologyNanotechnologyComputational biologyBiochemistryOrganic chemistryComputer scienceBiologyMaterials sciencePolymerEcologyProgramming languageChemical Synthesis and AnalysisClick Chemistry and ApplicationsAdvanced biosensing and bioanalysis techniques