2. Academic Validation
  3. The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing

The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing

  • Bioorg Med Chem Lett. 2008 Dec 15;18(24):6369-73. doi: 10.1016/j.bmcl.2008.10.102.
Clifford D Jones 1,  David M Andrews,  Andrew J Barker,  Kevin Blades,  Paula Daunt,  Simon East,  Catherine Geh,  Mark A Graham,  Keith M Johnson,  Sarah A Loddick,  Heather M McFarland,  Alexandra McGregor,  Louise Moss,  David A Rudge,  Peter B Simpson,  Michael L Swain,  Kin Y Tam,  Julie A Tucker,  Mike Walker
Affiliations

Affiliation

  • 1 Cancer and Infection Research, AstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. cliff.jones@astrazeneca.com
PMID: 18996007 DOI: 10.1016/j.bmcl.2008.10.102
Abstract

The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. Optimisation of inhibitory potency against multiple CDK's (1, 2 and 9) resulted in imidazole pyrimidine amides with potent in vitro anti-proliferative effects against a range of Cancer cell lines. Excellent physiochemical properties and large margins against inhibition of CYP isoforms and the hERG ion channel were achieved by modification of lipophilicity and amine basicity. A candidate with disease model activity in human Cancer cell line xenografts and with suitable physiochemical and pharmacokinetic profiles for intravenous (i.v.) dosing was selected for further development as AZD5597.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-50914
    98.09%, CDK抑制剂
    CDK
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