Hu, Liming published the artcileDesign, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors, HPLC of Formula: 1416437-27-8, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(23), 5830-5835, database is CAplus and MEDLINE.
A series of 4-((pyrazolo[1,5-a]pyrimidin-6-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide derivatives and 4-((imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide derivatives were designed, synthesized as new BCR-ABL tyrosine kinase inhibitors by using combinational strategies of scaffold hopping and conformational constraint. These new compounds were screened for BCR-ABL1 kinase inhibitory activity, and most showed good inhibitory activity against BCR-ABL1 kinase. One of the most potent compounds I strongly suppressed BCR-ABL1 kinase with IC50 value of 8.5 nM. The tested compounds I (and a second compound) showed strong inhibitory activities against K562 with IC50 value of less than 2 nM. Mol. docking studies indicated that these compounds fitted well with the active site of BCR-ABL1 protein. The results showed these inhibitors may serve as lead compounds for developing new drugs targeted at BCR-ABL kinase.
Bioorganic & Medicinal Chemistry Letters published new progress about 1416437-27-8. 1416437-27-8 belongs to pyrazoles-derivatives, auxiliary class Other Aromatic Heterocyclic,Boronic acid and ester,Boronate Esters,Boronic acid and ester, name is 6-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyrimidine, and the molecular formula is C12H16BN3O2, HPLC of Formula: 1416437-27-8.
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https://en.wikipedia.org/wiki/Pyrazole,
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