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Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors |
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| Authors: | 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 |
| Institution: | Department of Biology, Sunesis Pharmaceuticals, Inc., 395 Oyster Point Boulevard Suite 400, South San Francisco, CA 94080, USA. rfucini@sunesis.com |
| Abstract: | 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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