Author/Authors :
Emily J. Hanan، نويسنده , , Raymond V. Fucini، نويسنده , , Michael J. Romanowski، نويسنده , , Robert A. Elling and David K. Wilson، نويسنده , , Willard Lew، نويسنده , , Hans E. Purkey، نويسنده , , Erica C. VanderPorten، نويسنده , , Wenjin Yang، نويسنده ,
Abstract :
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.
Keywords :
kinase inhibitor , 2-Amino-isoxazolopyridines , Polo-like kinase (Plk) , SAR
