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Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52.

Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.

Author information

1
Cancer Research, AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.

Abstract

Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK activity, the SAR of the two series differs significantly. Protein inhibitor structure determination has confirmed differences in binding mode and given some understanding of these differences in SAR. Potent and selective imidazo[1,2-b]pyridazine inhibitors of CDK2 have been identified, which show >1 microM plasma levels following a 2mg/kg oral dose to mice.

PMID:
15081018
DOI:
10.1016/j.bmcl.2004.02.008
[Indexed for MEDLINE]

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