A unified "top-down" approach for the synthesis of diverse lead-like molecular scaffolds. (15th April 2022)

• Record Type: Journal Article
• Authors: Townley, Chloe; McMurray, Lindsay; Marsden, Stephen P.; Nelson, Adam
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 62(2022)
• Publication Date: 2022-04-15
• Subjects: Molecular diversity -- Molecular scaffolds -- Screening compounds; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2022.128631
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A "top-down" synthetic approach enabled the step-efficient synthesis of 21 diverse novel molecular scaffolds. The scaffolds were derived from four complex intermediates that had been prepared using cycloaddition chemistry. Scaffold-hopping of these intermediates was achieved through attachment of an additional ring, ring cleavage, ring expansion and/or ring fusion. It was shown that the resulting scaffolds could be decorated to yield diverse lead-like screening compounds.