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

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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.

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

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Article information


Submitted
17 Dec 2019
Accepted
20 Jan 2020
First published
20 Jan 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

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

A. R. Hanby, N. S. Troelsen, T. J. Osberger, S. L. Kidd, K. T. Mortensen and D. R. Spring, Chem. Commun., 2020, Advance Article , DOI: 10.1039/C9CC09796A

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