Aimon, A, Karageorgis, G orcid.org/0000-0001-5088-6047, Masters, J et al. (12 more authors) (2018) Realisation of small molecule libraries based on frameworks distantly related to natural products. Organic and Biomolecular Chemistry, 16 (17). pp. 3160-3167. ISSN 1477-0520
Abstract
The availability of high-quality screening compounds is of paramount importance for the discovery of innovative new medicines. Natural product (NP) frameworks can inspire the design of productive compound libraries. Here, we describe the design and synthesis of four compound libraries based on scaffolds that have broad NP-like features, but that are only distantly related to specific NPs. The optimisation of syntheses of the scaffolds using [5 + 2] cycloaddition chemistry is detailed, together with methods to yield exemplar decorated screening compounds. In each case, a library was nominated for production, leading to a total of >2900 screening compounds that augmented the Joint European Compound Library of the European Lead Factory.
Metadata
Item Type: | Article |
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Authors/Creators: |
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Copyright, Publisher and Additional Information: | (c) The Royal Society of Chemistry 2018. This is an author produced version of a paper published in Organic & Biomolecular Chemistry. Uploaded in accordance with the publisher's self-archiving policy. |
Dates: |
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Institution: | The University of Leeds |
Academic Units: | The University of Leeds > Faculty of Engineering & Physical Sciences (Leeds) > School of Chemistry (Leeds) > Organic Chemistry (Leeds) |
Funding Information: | Funder Grant number EU - European Union 115489-EUC2LID EU - European Union 115489-EUC2LID |
Depositing User: | Symplectic Publications |
Date Deposited: | 10 Apr 2018 16:34 |
Last Modified: | 11 Apr 2019 00:42 |
Status: | Published |
Publisher: | Royal Society of Chemistry |
Identification Number: | 10.1039/C8OB00688A |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:129449 |