2. Academic Validation
  3. Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5487-92. doi: 10.1016/j.bmcl.2008.09.024.
Malcolm Anderson 1,  David M Andrews,  Andy J Barker,  Claire A Brassington,  Jason Breed,  Kate F Byth,  Janet D Culshaw,  M Raymond V Finlay,  Eric Fisher,  Helen H J McMiken,  Clive P Green,  Dave W Heaton,  Ian A Nash,  Nicholas J Newcombe,  Sandra E Oakes,  Richard A Pauptit,  Andrew Roberts,  Judith J Stanway,  Andrew P Thomas,  Julie A Tucker,  Mike Walker,  Hazel M Weir
Affiliations

Affiliation

  • 1 AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
PMID: 18815031 DOI: 10.1016/j.bmcl.2008.09.024
Abstract

An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been developed. Protein inhibitor structure determination has provided an understanding of the emerging structure activity trends for the imidazole series. The introduction of a methyl sulfone at the aniline terminus led to a more orally bioavailable CDK Inhibitor that was progressed into clinical development.

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