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  • Title: Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins.
    Author: Bailly C, Bal C, Barbier P, Combes S, Finet JP, Hildebrand MP, Peyrot V, Wattez N.
    Journal: J Med Chem; 2003 Dec 04; 46(25):5437-44. PubMed ID: 14640552.
    Abstract:
    A series of A-ring polymethoxylated neoflavonoids was prepared by ligand coupling reactions involving either Suzuki or Stille reactions. Cytotoxicity studies indicated a potent activity against a CEM leukemia cell line for the compounds presenting a substitution pattern related to that of combretastatin A-4. The two compounds having a 3'-OH and a 4'-OCH(3) substituents on the 4-phenyl B-ring have no effect on human topoisomerases I and II but potently inhibit, in vitro, microtubule assembly. At the cell level, the active compounds were characterized as proapoptotic agents, but they can also trigger cell death via a nonapoptotic pathway.
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