Fsp3-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery

Abigail R Hanby; Nikolaj Sten Troelsen; Thomas J. Osberger; Sarah L Kidd; Kim T. Mortensen; David R Spring

doi:10.1039/c9cc09796a

Fsp³-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery

Abigail R Hanby, Nikolaj Sten Troelsen, Thomas J. Osberger, Sarah L Kidd, Kim T. Mortensen, David R Spring^*

^*Corresponding author for this work

Department of Chemistry

University of Cambridge

Research output: Contribution to journal › Journal article › Research › peer-review

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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.

Original language	English
Article number	2280
Journal	Chemical Communications
Volume	56
Number of pages	4
ISSN	1359-7345
DOIs	https://doi.org/10.1039/c9cc09796a
Publication status	Published - 2020

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Cite this

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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.",

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