Fsp<sup>3</sup>-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery.

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

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

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

Afiliação

Hanby AR; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk.
Troelsen NS; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk and Center for Nanomedicine and Theranostics, Department of Chemistry, Technical University of Denmark (DTU), Denmark.
Osberger TJ; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk and Department of Chemistry, California State Polytechnic University, Pomona, USA.
Kidd SL; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk and School of Chemistry, University of Leeds, Woodhouse Lane, Leeds, UK.
Mortensen KT; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk.
Spring DR; Department of Chemistry, University of Cambridge, Lensfield Rd, Cambridge, UK. spring@ch.cam.ac.uk.

Chem Commun (Camb) ; 56(15): 2280-2283, 2020 Feb 20.

Article em En | MEDLINE | ID: mdl-31984987

ABSTRACT

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.

Assuntos

Produtos Biológicos/química; Descoberta de Drogas; Bibliotecas de Moléculas Pequenas/química; Produtos Biológicos/síntese química; Estrutura Molecular; Bibliotecas de Moléculas Pequenas/síntese química

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Produtos Biológicos / Bibliotecas de Moléculas Pequenas / Descoberta de Drogas Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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