Pastor, Richard M. published the artcileDiscovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors, Related Products of pyrazoles-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(11), 2448-2452, database is CAplus and MEDLINE.
There is evidence that small mol. inhibitors of the nonreceptor tyrosine kinase ITK, a component of the T-cell receptor signaling cascade, could represent a novel asthma therapeutic class. Moreover, given the expected chronic dosing regimen of any asthma treatment, highly selective as well as potent inhibitors would be strongly preferred in any potential therapeutic. Here the authors report hit-to-lead optimization of a series of indazoles, e.g. I [R = Et, HOCH2, Me2NCH2CH2, etc.] that demonstrate sub-nanomolar inhibitory potency against ITK with strong cellular activity and good kinase selectivity. The authors also elucidate the binding mode of these inhibitors by solving the x-ray crystal structures of the complexes.
Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Related Products of pyrazoles-derivatives.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics