The invention discloses a sulfo-imidazolidone derivative as well as a synthesis method and application thereof. The sulfo-imidazolidone derivative has a structural formula 11 as shown in the specification and is prepared from solutions of substituted 2-mercaptobenzothiazole, aromatic aldehyde, isocyanide and malononitrile through stirring at the room temperature under catalysis of a binaphthol-Troger's base amine Schiff base derivative. The sulfo-imidazolidone derivative disclosed by the invention has a good inhibition effect on triple negative breast cancer (MDA-MB-231), breast cancer (MCF-7)and human lung cancer (A549) cell strains, in addition is low in toxicity upon normal human cells and has wide application prospects in preparing a new generation of anti-lung cancer and breast cancer specific medicines.