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Synthesis, X-ray crystal structure and tubulin-binding properties of a benzofuran analogue of the potent cytotoxic agent combretastatin A4

  1. Author:
    Banwell, M. G.
    Flynn, B. L.
    Willis, A. C.
    Hamel, E.

  2. Author Address

    Banwell MG Australian Natl Univ, Res Sch Chem, Inst Adv Studies Canberra ACT 0200 Australia Australian Natl Univ, Res Sch Chem, Inst Adv Studies Canberra ACT 0200 Australia NCI, Lab Drug Discovery Res & Dev, Dev Therapeut Program,Div Canc Treatment & Diag, Frederick Canc Res & Dev Ctr Frederick, MD 21702 USA
    1. Year: 1999
  2. Journal: Australian Journal of Chemistry
    1. 52
    2. 8
    3. Pages: 767-774
  4. Type of Article: Article
  1. Abstract:

    The benzofuran (4), a ring-fused analogue of the potent antimitotic agent combretastatin A4 (1), has been prepared by a convergent route involving 5-endo-dig iodocyclization of o-hydroxytolan (5) as the key step. Compound (4), which has been characterized crystallographically as well as spectroscopically, is inactive as a tubulin-binding agent. [References: 44]

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