Chemical Name:N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazo
linyl]amino]phenyl]benzamide
Biological Activity:
Novel, selective ATP-competitive inhibitor of
Aurora B kinase in vitro (IC50 values are 50, 250 and 1000 nM for
Aurora B, C and A kinases respectively). Selective over a range of other
kinases including cdk1 and PLK1 (IC50 > 10 μM). Inhibits
cell division and displays selective toxicity towards proliferating tumour
cells versus non-dividing cells.
Ditchfieldet al
(2003) Aurora B couples chromosome alignment with anaphase by targeting BubR1,
Mad2, and Cenp-E to kinetochores. J.Cell Bio. 161 267. Junget al (2006) Discovery of novel and potent thiazoloquinazolines as
selective Aurora A and B kinase inhibitors. J.Med.Chem. 49 955. Girdleret al (2006) Validating Aurora B as an anti-cancer drug target. J.Cell
Sci. 119 3664.