Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2 and Pim-3 protein kinases
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Nishiguchi, Gisele, Atallah, Gordana, Bellamacina, Cornelia, Burger, Matthew, Feucht, Paul, Garcia, Pablo, Han, Wooseok, Klivansky, Liana, Ding, Yu and Lindvall, Mika (2011) Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2 and Pim-3 protein kinases. Bioorganic and Medicinal Chemistry Letters, 21 (21). pp. 6366-6369.
Abstract
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: IC50 ≤ 2 nM and Pim-2: IC50 ≤ 100 nM).
| Item Type: | Article |
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| Additional Information: | author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Pim-kinase inhibitors; Indole; Kinase selectivity; Oncology |
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| Date Deposited: | 13 Oct 2015 13:15 |
| Last Modified: | 13 Oct 2015 13:15 |
| URI: | https://oak.novartis.com/id/eprint/4631 |