- Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin.
Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin.
Organic & biomolecular chemistry (2006-02-24)
Carine Aubry, A James Wilson, Paul R Jenkins, Sachin Mahale, Bhabatosh Chaudhuri, Jean-Didier Maréchal, Michael J Sutcliffe
PMID16493461
RÉSUMÉ
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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Millipore
Agarose−glutathion, set of 3 pre-packed columns (2.5 ml each), (1:1 suspension in a 0.5 M NaCl + 20% ethanol solution)