Deng, Xianming published the artcileExpanding the Diversity of Allosteric Bcr-Abl Inhibitors, Category: pyrazoles-derivatives, the publication is Journal of Medicinal Chemistry (2010), 53(19), 6934-6946, database is CAplus and MEDLINE.
Inhibition of Bcr-Abl kinase activity by imatinib for the treatment of chronic myeloid leukemia (CML) currently serves as the paradigm for targeting dominant oncogenes with small mols. The discovery of GNF-2 (I, R = H) and GNF-5 (I, R = CH2CH2OH) was recently reported as selective non-ATP competitive inhibitors of cellular Bcr-Abl kinase activity that target the myristate binding site. Herein is used cell-based structure-activity relationships to guide the optimization and diversification of ligands that are capable of binding to the myristate binding site and rationalize the findings based upon an Abl-compound I (R = H) cocrystal. The structure-activity relationships required to obtain potent antiproliferative activity against Bcr-Abl transformed cells is elucidated, and the discovery of new compounds II (R1 = 4-(NH2SO2)C6H4, 4-(MeSO2NH)C6H4, 4-pyrazolyl), III, and IV that display improved potency or pharmacol. properties is reported. This work demonstrates that a variety of structures can effectively target the Bcr-Abl myristate binding site and provides new leads for developing drugs that can target this binding site.
Journal of Medicinal Chemistry 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