| Autor: |
Destro, Lorenza, Van Melsen, Ross, Gobbi, Alex, Terzi, Andrea, Genitoni, Matteo, Zambon, Alfonso |
| Předmět: |
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| Zdroj: |
Applied Biosciences; Mar2022, Vol. 1 Issue 1, p64-72, 9p |
| Abstrakt: |
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). [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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