Design of Potent and Selective Hybrid Inhibitors of the Mitotic Kinase Nek2: Structure鈥揂ctivity Relationship, Structural Biology, and Cellular Activity
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- 作者：Paolo Innocenti ; Kwai-Ming J. Cheung ; Savade Solanki ; Corine Mas-Droux ; Fiona Rowan ; Sharon Yeoh ; Kathy Boxall ; Maura Westlake ; Lisa Pickard ; Tara Hardy ; Joanne E. Baxter ; G. Wynne Aherne ; Richard Bayliss ; Andrew M. Fry ; Swen Hoelder
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：April 12, 2012
- 年：2012
- 卷：55
- 期：7
- 页码：3228-3241
- 全文大小：579K
- 年卷期：v.55,no.7(April 12, 2012)
- ISSN：1520-4804
文摘
We report herein a series of Nek2 inhibitors based on an aminopyridine scaffold. These compounds have been designed by combining key elements of two previously discovered chemical series. Structure based design led to aminopyridine (R)-21, a potent and selective inhibitor able to modulate Nek2 activity in cells.