Article
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Bioorganic & medicinal chemistry letters - 15 Oct 2008
Fucini Raymond V, Hanan Emily J, Romanowski Michael J, Elling Robert A, Lew Willard, Barr Kenneth J, Zhu Jiang, Yoburn Joshua C, Liu Yang, Fahr Bruce T, Fan Junfa, Lu Yafan, Pham Phuongly, Choong Ingrid C, VanderPorten Erica C, Bui Minna, Purkey Hans E, Evanchik Marc J, Yang Wenjin
Abstract excerpt
A series of 2-amino-pyrazolopyridines was designed and synthesized as Polo-like kinase (Plk) inhibitors based on a low micromolar hit. The SAR was developed to provide compounds exhibiting low nanomolar inhibitory activity of Plk1; the phenotype of treated cells is consistent with Plk1 inhibition. A co-crystal structure of one of these compounds with zPlk1 confirms an ATP-competitive binding mode.
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