| Literature DB >> 18793847 |
Raymond V Fucini1, Emily J Hanan, Michael J Romanowski, Robert A Elling, Willard Lew, Kenneth J Barr, Jiang Zhu, Joshua C Yoburn, Yang Liu, Bruce T Fahr, Junfa Fan, Yafan Lu, Phuongly Pham, Ingrid C Choong, Erica C VanderPorten, Minna Bui, Hans E Purkey, Marc J Evanchik, Wenjin Yang.
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.Entities:
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Year: 2008 PMID： 18793847 DOI： 10.1016/j.bmcl.2008.08.095
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823