Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 4, Issue 24, Pages 4478-4484Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/b613861f
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The design, synthesis and biological activity of a series of non-planar dihydro-beta-carboline and beta-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 mu 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.
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