Phenotype-directed discovery of diverse, biologically-relevant molecular scaffolds†

Abstract

An array of reactions of diazo substrates with many possible outcomes was executed, and the biological relevance of the resulting products assessed in the cell painting assay. Reactions that had yielded bioactive products were scaled-up, and the products structurally elucidated. By bypassing the need to characterise all reaction products, this phenotype-directed approach enabled efficient discovery of functionally-distinctive molecules based on novel, structurally-diverse scaffolds.