Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin |
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| Authors: | Aubry Carine Wilson A James Jenkins Paul R Mahale Sachin Chaudhuri Bhabatosh Maréchal Jean-Didier Sutcliffe Michael J |
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| Institution: | Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK. kin@le.ac.uk |
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| 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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