Highly Potent, Selective, and Orally Bioavailable 4‑Thiazol‑N‑(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation

Cyclin D dependent kinases (CDK4 and CDK6) regulate entry into S phase of the cell cycle and are validated targets for anticancer drug discovery. Herein we detail the discovery of a novel series of 4-thiazol-N-(pyridin-2-yl)­pyrimidin-2-amine derivatives as highly potent and selective inhibitors of...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-03, Vol.60 (5), p.1892-1915
Hauptverfasser:	Tadesse, Solomon, Yu, Mingfeng, Mekonnen, Laychiluh B, Lam, Frankie, Islam, Saiful, Tomusange, Khamis, Rahaman, Muhammed H, Noll, Benjamin, Basnet, Sunita K. C, Teo, Theodosia, Albrecht, Hugo, Milne, Robert, Wang, Shudong
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Biological Availability Cell Line, Tumor Cyclin-Dependent Kinase 4 - antagonists & inhibitors Cyclin-Dependent Kinase 6 - antagonists & inhibitors Cyclin-Dependent Kinases - antagonists & inhibitors Drug Design Humans Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship
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