• Bioorg. Med. Chem. Lett. · Dec 2013

    Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.

    • Kevin Anderson, Yi Chen, Zhi Chen, Romyr Dominique, Kelli Glenn, Yang He, Cheryl Janson, Kin-Chun Luk, Christine Lukacs, Ann Polonskaia, Qi Qiao, Aruna Railkar, Pamela Rossman, Hongmao Sun, Qing Xiang, Masha Vilenchik, Peter Wovkulich, and Xiaolei Zhang.
    • Discovery Chemistry, Hoffmann-La Roche Inc., pRED, Pharma Research & Early Development, 340 Kingsland Street, Nutley, NJ 07110, USA.
    • Bioorg. Med. Chem. Lett. 2013 Dec 15; 23 (24): 6610-5.

    AbstractDYRK1B is a kinase over-expressed in certain cancer cells (including colon, ovarian, pancreatic, etc.). Recent publications have demonstrated inhibition of DYRK1B could be an attractive target for cancer therapy. From a data-mining effort, the team has discovered analogues of pyrido[2,3-d]pyrimidines as potent enantio-selective inhibitors of DYRK1B. Cells treated with a tool compound from this series showed the same cellular effects as down regulation of DYRK1B with siRNA. Such effects are consistent with the proposed mechanism of action. Progress of the SAR study is presented. Copyright © 2013 Elsevier Ltd. All rights reserved.

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