Fsp<sup>3</sup>-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery
Abigail R. Hanby, Nikolaj S. Troelsen, Thomas J. Osberger, Sarah L. Kidd, Kim T. Mortensen, David R. Spring
Abstract
Herein, we describe the natural product inspired synthesis of 38 complex small molecules based upon 20 unique frameworks suitable for fragment-based screening. Utilising an efficient strategy, two key building block diastereomers were harnessed to generate novel, three-dimensional fragments which each possess numerous synthetically accessible fragment growth positions.
Topics & Concepts
Fragment (logic)Drug discoveryNatural productCombinatorial chemistryChemistrySmall moleculeProduct (mathematics)Computer scienceStereochemistryAlgorithmMathematicsBiochemistryGeometryChemical Synthesis and AnalysisMicrobial Natural Products and BiosynthesisClick Chemistry and Applications