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Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold

Nishiguchi, Gisele and Burger, Matthew and Han, Wooseok and Tamez Jr., Victoriano and Lindvall, Mika and Bellamacina, Cornelia and Feucht, Paul and Wong, Kent and Lan, Jiong and Atallah, Gordana and Ding, Yu and Garcia, Pablo and Zavorotinskaya, Tatiana and Dai, Yumin (2016) Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold. Bioorganic and Medicinal Chemistry Letters, 26 (9). pp. 2328-2332. ISSN 1464-3405

Abstract

The Pim proteins (1, 2 and 3) are serine/threonine kinases that have been found to be upregulated in many hematological malignancies and solid tumors. As a result of overlapping functions among the three isoforms, inhibition of all three Pim kinases has become an attractive strategy for cancer therapy. Herein we describe our efforts in identifying potent pan-PIM inhibitors that are derived from our previously reported pyridyl carboxamide scaffold as part of a medicinal chemistry strategy to address metabolic stability.

Item Type: Article
Keywords: Hematological malignancies pan-PIM kinase inhibitor Pim kinase
Date Deposited: 13 Mar 2018 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/28047

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