Publication Abstract from PubMed
A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by structure-based drug design, SAR of the series afforded a highly selective indole chemotype that was further developed into a potent set of compounds against Pim-1, 2, and 3 (Pim-1 and Pim-3: IC(50)</=2nM and Pim-2: IC(50)</=100nM).
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.,Nishiguchi GA, Atallah G, Bellamacina C, Burger MT, Ding Y, Feucht PH, Garcia PD, Han W, Klivansky L, Lindvall M Bioorg Med Chem Lett. 2011 Nov 1;21(21):6366-9. Epub 2011 Sep 10. PMID:21945284[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
