2. Academic Validation
  3. Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors

Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9. doi: 10.1016/j.bmcl.2008.10.075.
Clifford D Jones 1,  David M Andrews,  Andrew J Barker,  Kevin Blades,  Kate F Byth,  M Raymond V Finlay,  Catherine Geh,  Clive P Green,  Marie Johannsen,  Mike Walker,  Hazel M Weir
Affiliations

Affiliation

  • 1 Cancer and Infection Research, AstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. cliff.jones@astrazeneca.com
PMID: 18986805 DOI: 10.1016/j.bmcl.2008.10.075
Abstract

The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative effects against Cancer cell lines. Control of overall lipophilicity was important to achieve good in vitro potency along with acceptable physiochemical properties and margins against inhibition of both CYP isoforms and the hERG potassium ion channel. A compound with an attractive overall balance of properties was profiled in vivo and possessed suitable physiochemical and pharmacokinetic profiles for oral dosing.

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