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J Med Chem. 2012 Apr 12;55(7):3228-41. doi: 10.1021/jm201683b. Epub 2012 Mar 23.

Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity.

Author information

1
Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom.

Abstract

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.

PMID:
22404346
PMCID:
PMC3935458
DOI:
10.1021/jm201683b
[Indexed for MEDLINE]
Free PMC Article

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