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- Title
Expedient Access to Type II Kinase Inhibitor Chemotypes by Microwave-Assisted Suzuki Coupling.
- Authors
Destro, Lorenza; Van Melsen, Ross; Gobbi, Alex; Terzi, Andrea; Genitoni, Matteo; Zambon, Alfonso
- Abstract
Functionalized pyrazole-urea scaffolds are a common type II chemotype for the inhibition of protein kinases (PKs), binding simultaneously into the ATP-binding pocket with an ATP bioisostere and into a vicinal allosteric pocket with a pyrazole group. Standard approaches to the scaffold require multi-step synthesis of the ATP bioisostere followed by phosgene or triphosgene-mediated coupling with the substituted pyrazole group. Here we report an expedient approach to the chemotype, characterized by an optimized MW-assisted Suzuki coupling on easily accessed bromo-phenyl pyrazole ureas. The new protocol allowed quick access a large library of target analogues covering a broad chemical space of putative protein kinases inhibitors (PKIs).
- Subjects
KINASE inhibitors; ADENOSINE triphosphate; PYRAZOLES; PROTEIN kinases; PHOSGENE
- Publication
Applied Biosciences, 2022, Vol 1, Issue 1, p64
- ISSN
2813-0464
- Publication type
Article
- DOI
10.3390/applbiosci1010004