Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 25, Issue 68, Pages 15498-15503Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201904175
Keywords
branching pathway; cell painting; folding pathway; mitotic inhibitors; sulfonamides
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Funding
- Max Planck Society
- Innovative Medicines Initiative Joint Undertaking [115489]
- European Union's Seventh Framework Programme (FP7/2007-2013)
- EFPIA companies
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A branching-folding synthetic strategy that affords a range of diverse cyclic benzo-sulfonamide scaffolds is presented. Whereas different annulation reactions on common ketimine substrates build the branching phase of the scaffold synthesis, a common hydrogenative ring-expansion method, facilitated by an increase of the ring-strain during the branching phase, led to sulfonamides bearing medium-sized rings in a folding pathway. Cell painting assay was successfully employed to identify tubulin targeting sulfonamides as novel mitotic inhibitors.
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