Synthesis and Biological Evaluation of 4-Arylcoumarin Analogues of Combretastatins
Journal of Medicinal Chemistry2003Vol. 46(25), pp. 5437–5444
Citations Over TimeTop 12% of 2003 papers
Christian Bailly, Christine Bal, Pascale Barbier, Sébastien Combes, Jean‐Pierre Finet, Marie‐Paule Hildebrand, Vincent Peyrot, Nicole Wattez
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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