1453852-02-2Relevant academic research and scientific papers
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2
Ren, Li,Grina, Jonas,Moreno, David,Blake, James F.,Gaudino, John J.,Garrey, Rustam,Metcalf, Andrew T.,Burkard, Michael,Martinson, Matthew,Rasor, Kevin,Chen, Huifen,Dean, Brian,Gould, Stephen E.,Pacheco, Patricia,Shahidi-Latham, Sheerin,Yin, Jianping,West, Kristina,Wang, Weiru,Moffat, John G.,Schwarz, Jacob B.
, p. 1976 - 1991 (2015/04/27)
Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation.
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00272, (2013/09/12)
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
