1386979-05-0Relevant articles and documents
Pyrido[2,3-d]pyrimidines: Discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors
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
, p. 6610 - 6615 (2014/01/06)
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 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.
PYRIDO PYRIMIDINES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
