Title of article
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors
Author/Authors
Raymond V. Fucini، نويسنده , , Emily J. Hanan، نويسنده , , Michael J. Romanowski، نويسنده , , Robert A. Elling and David K. Wilson، نويسنده , , Willard Lew، نويسنده , , Kenneth J. Barr، نويسنده , , Jiang Zhu، نويسنده , , Joshua C. Yoburn، نويسنده , , Yang Liu، نويسنده , , Bruce T. Fahr، نويسنده , , Junfa Fan، نويسنده , , Yafan Lu، نويسنده , , Phuongly Pham، نويسنده , , Ingrid C. Choong، نويسنده , , Erica C. VanderPorten، نويسنده , , Minna Bui، نويسنده , , Hans E. Purkey، نويسنده , , Marc J. Evanchik، نويسنده , , Wenjin Yang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
5648
To page
5652
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.
Keywords
SAR , kinase inhibitor , Polo-like kinase (Plk) , 2-Amino-pyrazolopyridine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800078
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