The invention belongs to the technical field of medicine and discloses diosgenin anti-tumor derivative and a synthesizing method thereof. The synthesizing method comprises the steps: after compound 3is obtained, utilizing triethylamine as alkali to react with chloroacetyl chloride to obtain 3-Csite amide compound 4; finally, reacting the compound 4 with nitrogen-containing compound to obtain a series of amide nitrogen-containing compound 5. The derivative disclosed by the invention and intermediates of the derivative wholly show high inhibitory activity and low cytotoxicity, the derivative 5aand 5e containing piperazine and the intermediate 4 show stronger inhibitory activity, and the derivative 5c, 5e, 5f, 5g, 5h and 5i shows low cytotoxicity to HBE cells. The results of the derivativedisclosed by the invention can provide certain reference value for structural modification of the diosgenin and analysis of anti-tumor activity of different radicals.