2. Academic Validation
  3. SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. doi: 10.1016/j.bmcl.2005.11.053.
Nicola M Heron 1,  Malcolm Anderson,  David P Blowers,  Jason Breed,  Jonathan M Eden,  Stephen Green,  George B Hill,  Trevor Johnson,  Frederic H Jung,  Helen H J McMiken,  Andrew A Mortlock,  Andrew D Pannifer,  Richard A Pauptit,  Jennifer Pink,  Nicola J Roberts,  Siân Rowsell
Affiliations

Affiliation

  • 1 AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG,UK. [email protected]
PMID: 16337122 DOI: 10.1016/j.bmcl.2005.11.053
Abstract

A novel series of 5-aminopyrimidinyl quinazolines has been developed from anilino-quinazoline 1, which was identified in a high throughput screen for Aurora A. Introduction of the pyrimidine ring and optimisation of the substituents both on this ring and at the C7 position of the quinazoline led to the discovery of compounds that are highly specific Aurora Kinase inhibitors. Co-crystallisation of one of these inhibitors with a fragment of Aurora A shows the importance of the benzamido group in achieving selectivity.

Figures
Products