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

…, A Polonskaia, Q Qiao, A Railkar, P Rossman…

Index: Anderson, Kevin; Chen, Yi; Chen, Zhi; Dominique, Romyr; Glenn, Kelli; He, Yang; Janson, Cheryl; Luk, Kin-Chun; Lukacs, Christine; Polonskaia, Ann; Qiao, Qi; Railkar, Aruna; Rossman, Pamela; Sun, Hongmao; Xiang, Qing; Vilenchik, Masha; Wovkulich, Peter; Zhang, Xiaolei Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6610 - 6615

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Citation Number: 18

Abstract

Abstract DYRK1B 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 ...