Caldwell, John J. published the artcileDesign and synthesis of 2(1H)-pyrazinones as inhibitors of protein kinases, Category: pyrazoles-derivatives, the publication is Tetrahedron (2012), 68(47), 9713-9728, database is CAplus.
Kinase enzymes play a key role in the development and progression of cancer. Inhibitors of deregulated kinases are effective small mol. anticancer drugs. The 2(1H)-pyrazinone heterocycle is a previously unexploited motif that can fulfil the structural requirements for ATP-competitive inhibition of kinases. Rapid solution-phase syntheses of novel 3,5- and 3,6-disubstituted-2(1H)-pyrazinones were developed through selective, sequential substitution of 2,5-dihalo-3-benzyloxypyrazine and 3,5-dihalo-2(1H)-pyrazinone intermediates. Palladium-catalyzed cross-couplings and SNAr reactions were used to introduce substituents chosen on the basis of the calculated physicochem. properties of the target pyrazinones. Representative compounds, e.g., I, demonstrated good solubility, kinase inhibitory activity and antiproliferative activity in human tumor cells, confirming the suitability of this chem. class as a kinase-focused library.
Tetrahedron published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Category: pyrazoles-derivatives.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics