Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin
Carine Aubry1, A James Wilson, Paul R Jenkins
1Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK. kin@le.ac.uk
Organic & Biomolecular Chemistry
|February 24, 2006
Abstract:
We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound has an IC50 for the inhibition of CDK4 of 6 microM.
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