Incorporation of viridicatin alkaloid-like scaffolds into DNA-encoded chemical libraries

Thiazolidione, conferring drug-like properties, is an important heterocycle that widely exists in medicinally relevant molecules. In this work, by efficiently assembling various DNA-tagged primary amines, abundant aryl isothiocyanates, and ethyl bromoacetate, we present a DNA-compatible three-component annulation to generate a 2-iminothiazolidin-4-one scaffold, which was further decorated via Knoevenagel condensation by employing (hetero)aryl and alkyl aldehydes. These thiazolidione derivatives should find broad use in focused DNA-encoded library construction.

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Incorporation of viridicatin alkaloid-like scaffolds into DNA-encoded chemical libraries

Abstract: Viridicatin alkaloids as natural products have attracted great interest due to their unique core scaffold. To fully exploit their potential application in DNA-encoded chemical libraries-facilitating drug discovery, we here describe...

Cited by 2 publications

References 48 publications

Screening and evaluation of the hit compound from a DNA-encoded library derived from natural products based on immobilized endothelin receptor A

Screening and evaluation of the hit compound from a DNA-encoded library derived from natural products based on immobilized endothelin receptor A

DNA-Compatible Synthesis of Thiazolidione Derivatives via Three-Component Annulation and Knoevenagel Condensation

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