Okolo, EA, Pahl, A, Sievers, S et al. (3 more authors) (2023) Scaffold Remodelling of Diazaspirotricycles Enables Synthesis of Diverse sp3-Rich Compounds With Distinct Phenotypic Effects. Chemistry: A European Journal, 29 (26). e202203992. ISSN 0947-6539
Abstract
A ‘top down’ scaffold remodelling approach to library synthesis was applied to spirotricyclic ureas prepared by a complexity-generating oxidative dearomatisation. Eighteen structurally-distinct, sp3-rich scaffolds were accessed from the parent tricycle through ring addition, cleavage and expansion strategies. Biological screening of a small compound library based on these scaffolds using the cell-painting assay demonstrated distinctive phenotypic responses engendered by different library members, illustrating the functional as well as structural diversity of the compounds.
Metadata
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Copyright, Publisher and Additional Information: | © 2023 The Authors. Chemistry- A European Journal published by Wiley-VCHGmbH. This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution andre-production in any medium, provided the original work is properly cited. | ||||
Keywords: | dearomatisation; library synthesis; molecular diversity; oxidation; phenotypic screening | ||||
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: |
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Depositing User: | Symplectic Publications | ||||
Date Deposited: | 16 Feb 2023 16:49 | ||||
Last Modified: | 26 Jul 2023 14:51 | ||||
Published Version: | https://chemistry-europe.onlinelibrary.wiley.com/d... | ||||
Status: | Published | ||||
Publisher: | Wiley | ||||
Identification Number: | https://doi.org/10.1002/chem.202203992 |