The invention belongs to the field of antineoplastic compounds and relates to a water-soluble derivative of diphenylethene compounds, especially a water-soluble derivative of trans-4-[2-(3,5-dimethoxyphenyl)vinyl]-1,2-benzenediol as shown in the formula I, a preparation method and a usage thereof in the preparation of antitumor drugs. The water-soluble derivative of diphenylethene compounds is prepared through water-soluble reconstruction by taking the compound, trans-4-[2-(3,5- dimethoxyphenyl)vinyl]-1,2-benzenediol, as a parent nucleus. Results of in vitro antineoplastic tests show that the water-soluble derivative of diphenylethene compounds has significant effects in inhibiting brain glioma cells SF188 and U87wt, breast cancer cells MCF-7wt and large cell lung cancer cells H460. The activity of the cells decreases along with the increase of drug concentration. The derivative disclosed by the invention is an effective antitumor agent and further, the derivative can be used for preparing the antitumor drugs.