2c4g

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Revision as of 16:54, 29 October 2007

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spinqualitylabelsall models 2c4g, resolution 2.70Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514

Overview

We have recently reported about a new class of Aurora-A inhibitors based, on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. Here we describe, the synthesis and early expansion of CDK2/cyclin A-E inhibitors belonging, to the same chemical class. Synthesis of the compounds was accomplished, using a solution-phase protocol amenable to rapid parallel expansion., Compounds with nanomolar activity in the biochemical assay and able to, efficiently inhibit CDK2-mediated tumor cell proliferation have been, obtained.

About this Structure

2C4G is a [Protein complex] structure of sequences from [Homo sapiens] with SO4 and 514 as [ligands]. Active as [[1]], with EC number [2.7.1.37]. Full crystallographic information is available from [OCA].

Reference

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors., Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittala V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG, Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14. PMID:16290148

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