The present invention disclosed a class of new derivatives of CombretastatinofFormula (I) obtained by total synthesis. The strategy developed for each ofthe compounds, isto introduce a fluoroalkoxy to the 4'- position of the B aromatic ring innatural productCombretastatin, and meanwhile, functionally chemically modify the 3'-positionwith amino,nitro, halogen, alkoxy, phosphate, side chain of an amino acid etc. ComparedtoCombretastatin 4, said compounds show more activity in inhibiting the assemblyof tubulininto microtubules, and are useful as antitumor agent and/or anti-angiogenicagent.(see formula I)