Song, Pinrao; Chen, Ming; Ma, Xiaodong; Xu, Lei; Liu, Tao; Zhou, Yubo; Hu, Yongzhou published the artcile< Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold>, Application In Synthesis of 22280-62-2, the main research area is inhibitor Aurora pyrrolopyridinylindazole scaffold; Antiproliferative agents; Aurora A inhibitors; Cell cycle profile; Pyrrolopyridin-indazoles; Selectivity.
A novel series of 3-(pyrrolopyridin-2-yl)indazole derivatives were synthesized and biol. evaluated for their anti-proliferative effects on five human cancer cell lines. As a result, all of them exhibited vigorous potency against HL60 cell line with IC50 values ranging from singe digital nanomolar to micromolar level. Besides, a majority of them displayed modest to good antiproliferative activities against the other four cell lines, including KB, SMMC-7721, HCT116, and A549. Particularly, compound 2y, as the most distinguished one in this series, demonstrated IC50 values of 8.3 nM and 1.3 nM against HL60 and HCT116 cell lines, resp. Afterwards, for exploring the mol. target, compounds2d, 2g and 2y were further selected to evaluate the inhibitory activities against a panel of kinases. Finally, they were identified to be targeting Aurora A kinase with significant selectivity over other kinases, such as CHK1, CDK2, MEK1, GSK3β, BRAF, IKKβ and PKC.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Application In Synthesis of 22280-62-2.