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Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2 and Pim-3 protein kinases

Nishiguchi, Gisele and Atallah, Gordana and Bellamacina, Cornelia and Burger, Matthew and Feucht, Paul and Garcia, Pablo and Han, Wooseok and Klivansky, Liana and 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

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