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Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Abstract：

:The o-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC(50) = 6.1 ± 1.0 nM) from in-house screening. Detailed structure-activity relationship (SAR) studies indicated that polar substituents at the para position of the B-ring are critical for potent activity. X-ray crystallography studies revealed that compound 1 is a type I inhibitor that binds the Aurora kinase active site in a DFG-in conformation. Structure-activity guided replacement of the A-ring carboxylic acid with halogens and incorporation of fluorine at the pyrimidine 5-position led to highly potent inhibitors of Aurora A that bind in a DFG-out conformation. B-Ring modifications were undertaken to improve the solubility and cell permeability. Compounds such as 9m with water-solubilizing moieties at the para position of the B-ring inhibited the autophosphorylation of Aurora A in MDA-MB-468 breast cancer cells.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Lawrence HR,Martin MP,Luo Y,Pireddu R,Yang H,Gevariya H,Ozcan S,Zhu JY,Kendig R,Rodriguez M,Elias R,Cheng JQ,Sebti SM,Schonbrunn E,Lawrence NJ

doi

10.1021/jm300334d

subject

Has Abstract

pub_date

2012-09-13 00:00:00

pages

7392-7416

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

55

pub_type

杂志文章

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