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

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Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM

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. Epub 2008 Sep 10.

PubMed ID

18815031 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-[(4-Imidazo[1,2-a]Pyridin-3-Ylpyrimidin-2-Yl)Amino]Benzenesulfonamide	Cyclin-dependent kinase 2	IC 50 (nM)	2	N/A	N/A	Details
N-(2-METHOXYETHYL)-4-({4-[2-METHYL-1-(1-METHYLETHYL)-1H-IMIDAZOL-5-YL]PYRIMIDIN-2-YL}AMINO)BENZENESULFONAMIDE	Cyclin-dependent kinase 2	IC 50 (nM)	1	N/A	N/A	Details