Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.

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Stevens KL, Reno MJ, Alberti JB, Price DJ, Kane-Carson LS, Knick VB, Shewchuk LM, Hassell AM, Veal JM, Davis ST, Griffin RJ, Peel MR

Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5758-62. doi: 10.1016/j.bmcl.2008.09.069. Epub 2008 Sep 24.

PubMed ID

18835709 [ View in PubMed

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Abstract

A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3beta.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N-cyclopropyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine	Cyclin-dependent kinase 2	IC 50 (nM)	120	N/A	N/A	Details