Scaffold Remodelling of Diazaspirotricycles Enables Synthesis of Diverse sp 3 ‐Rich Compounds With Distinct Phenotypic Effects

A ‘top down’ scaffold remodelling approach to library synthesis was applied to spirotricyclic ureas prepared by a complexity‐generating oxidative dearomatisation. Eighteen structurally‐distinct, sp 3 ‐rich scaffolds were accessed from the parent tricycle through ring addition, cleavage and expansion...

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Veröffentlicht in:Chemistry : a European journal Jg. 29; H. 26; S. e202203992
Hauptverfasser: Okolo, Ephraim A., Pahl, Axel, Sievers, Sonja, Pask, Christopher M., Nelson, Adam, Marsden, Stephen P.
Format: Journal Article
Sprache:Englisch
Veröffentlicht: Germany 08.05.2023
Schlagworte:
Gene Library
Small Molecule Libraries - chemistry
phenotypic screening
library synthesis
molecular diversity
dearomatisation
ISSN:0947-6539, 1521-3765
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Zusammenfassung:A ‘top down’ scaffold remodelling approach to library synthesis was applied to spirotricyclic ureas prepared by a complexity‐generating oxidative dearomatisation. Eighteen structurally‐distinct, sp 3 ‐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.
ISSN:0947-6539
1521-3765
DOI:10.1002/chem.202203992