Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.

The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent… CONTINUE READING