Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors
The design, synthesis and biological activity of a series of non-planar dihydro-β-carboline and β-carboline-based derivatives of the toxic anticancer agent fascaplysin is presented. We show these compounds to be selective inhibitors of CDK4 over CDK2 with an IC50 (CDK4-cyclin D1) = 11 mol for the best compound in the series 4d. The crystallographic analysis of some of the compounds synthesised (3b/d and 4a-d) was carried out, in an effort to estimate the structural similarities between the designed inhibitors and the model compound fascaplysin. The Royal Society of Chemistry.
Garcia, Marcos D.,Wilson, A. James,Emmerson, Daniel P.G.,Jenkins, Paul R.,Mahale, Sachin,Chaudhuri, Bhabatosh
p. 4478 - 4484
(2008/09/19)
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