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

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

  • Bioorg Med Chem Lett. 2016 May 1;26(9):2328-32. doi: 10.1016/j.bmcl.2016.03.037.
Gisele A Nishiguchi 1,  Matthew T Burger 2,  Wooseok Han 2,  Jiong Lan 2,  Gordana Atallah 2,  Victoriano Tamez 2,  Mika Lindvall 2,  Cornelia Bellamacina 2,  Pablo Garcia 3,  Paul Feucht 3,  Tatiana Zavorotinskaya 3,  Yumin Dai 3,  Kent Wong 2
Affiliations

Affiliations

  • 1 Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, United States. Electronic address: gisele.nishiguchi@novartis.com.
  • 2 Global Discovery Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, United States.
  • 3 Oncology, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, United States.
PMID: 26995528 DOI: 10.1016/j.bmcl.2016.03.037
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.

Keywords

Hematological malignancies; Pim kinase; pan-PIM kinase inhibitor.

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