2c4g

From Proteopedia

Revision as of 15:53, 5 November 2007

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 Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Structure known Active Site: AC1. 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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