Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases

…, Y Dai, C Abad-Zapatero, DH Albert, JJ Bouska…

Index: McClellan, William J.; Dai, Yujia; Abad-Zapatero, Cele; Albert, Daniel H.; Bouska, Jennifer J.; Glaser, Keith B.; Magoc, Terry J.; Marcotte, Patrick A.; Osterling, Donald J.; Stewart, Kent D.; Davidsen, Steven K.; Michaelides, Michael R. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5620 - 5624

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Citation Number: 26

Abstract

As part of our effort to discover Aurora kinase inhibitors, a high throughput screen of the Abbott compound collection revealed that 1 was a potent inhibitor of both Aurora A and Aurora B (IC 50 = 20 and 15 nM, respectively, 100 μM ATP). As we tried to optimize this pyrrolopyrimidine template, we were interested in replacing the pyrrolopyrimidine core with a thienopyrimidine moiety (2), which has been shown by us to be a favorable structural template for kinase ...