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

…, C Mas-Droux, F Rowan, S Yeoh, K Boxall…

Index: Innocenti, Paolo; Cheung, Kwai-Ming J.; Solanki, Savade; Mas-Droux, Corine; Rowan, Fiona; Yeoh, Sharon; Boxall, Kathy; Westlake, Maura; Pickard, Lisa; Hardy, Tara; Baxter, Joanne E.; Aherne, G. Wynne; Bayliss, Richard; Fry, Andrew M.; Hoelder, Swen Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3228 - 3241

Full Text: HTML

Citation Number: 36

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.

Related Articles:

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity

[Glennon, Richard A.; Raghupathi, Reva; Bartyzel, Piotr; Teitler, Milt; Leonhardt, Sigrun Journal of Medicinal Chemistry, 1992 , vol. 35, # 4 p. 734 - 740]

Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human β3-adrenergic receptor agonists with good oral bioavailability. Part I

[Journal of Medicinal Chemistry, , vol. 51, # 6 p. 1925 - 1944]

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

[Journal of Medicinal Chemistry, , vol. 55, # 7 p. 3228 - 3241]

More Articles...