Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
Copyright policy )Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors
A series of 2-amino-isoxazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors. Key SAR and crystallographic data are discussed. More advanced analogues inhibit Plk1 with good enzymatic activity and modest cell-based activity. Differential selectivity among the three Plk isoforms is observed.
Molecular Structure, Pyridines, Molecular Conformation, Cell Cycle Proteins, Isoxazoles, Protein Serine-Threonine Kinases, Crystallography, X-Ray, Isoenzymes, Polo-Like Kinase 1, Structure-Activity Relationship, Drug Design, Proto-Oncogene Proteins, Microsomes, Liver, Combinatorial Chemistry Techniques, Humans, Drug Screening Assays, Antitumor
Molecular Structure, Pyridines, Molecular Conformation, Cell Cycle Proteins, Isoxazoles, Protein Serine-Threonine Kinases, Crystallography, X-Ray, Isoenzymes, Polo-Like Kinase 1, Structure-Activity Relationship, Drug Design, Proto-Oncogene Proteins, Microsomes, Liver, Combinatorial Chemistry Techniques, Humans, Drug Screening Assays, Antitumor
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