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Issue 24, 2006
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Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors

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Abstract

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 µmol for the best compound in the series 4d. The crystallographic analysis of some of the compounds synthesised (3b/d and 4ad) was carried out, in an effort to estimate the structural similarities between the designed inhibitors and the model compound fascaplysin.

Graphical abstract: Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors

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The article was received on 22 Sep 2006, accepted on 26 Oct 2006 and first published on 09 Nov 2006


Article type: Paper
DOI: 10.1039/B613861F
Citation: Org. Biomol. Chem., 2006,4, 4478-4484
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    Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors

    M. D. García, A. J. Wilson, D. P. G. Emmerson, P. R. Jenkins, S. Mahale and B. Chaudhuri, Org. Biomol. Chem., 2006, 4, 4478
    DOI: 10.1039/B613861F

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