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  • Title: Synthesis, crystal structure and biological activity of beta-carboline based selective CDK4-cyclin D1 inhibitors.
    Author: García MD, Wilson AJ, Emmerson DP, Jenkins PR, Mahale S, Chaudhuri B.
    Journal: Org Biomol Chem; 2006 Dec 21; 4(24):4478-84. PubMed ID: 17268643.
    Abstract:
    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 micromol 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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