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  • Title: Syntheses and biological evaluation of ring-C modified colchicine analogs.
    Author: Yang B, Zhu ZC, Goodson HV, Miller MJ.
    Journal: Bioorg Med Chem Lett; 2010 Jun 15; 20(12):3831-3. PubMed ID: 20529690.
    Abstract:
    Ring-C modified alkaloids were synthesized from colchicine using iminonitroso Diels-Alder reactions in a highly regio- and stereoselective fashion. Several analogs exhibited cytotoxic activity similar to that of colchicine itself against PC-3 and MCF-7 cancer cell lines, by serving as prodrugs of colchicine through retro Diels-Alder reactions under the assayed conditions. In vitro microtubule polymerization assays indicated that these modifications affected their interaction with tubulin.
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