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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Vydáno v:Chemistry : a European journal Ročník 29; číslo 26; s. e202203992
Hlavní autoři: Okolo, Ephraim A., Pahl, Axel, Sievers, Sonja, Pask, Christopher M., Nelson, Adam, Marsden, Stephen P.
Médium: Journal Article
Jazyk:angličtina
Vydáno: Germany 08.05.2023
Témata:
Gene Library
Small Molecule Libraries - chemistry
phenotypic screening
library synthesis
molecular diversity
dearomatisation
ISSN:0947-6539, 1521-3765
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Shrnutí: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