Eight novel silicon-containing diorganotin complexes with salicylaldehyde thiosemicarbazone were synthesized. They were characterized by 1 H NMR, 13 C NMR, IR spectra, elemental analysis and X-ray singlecrystal diffraction. Spectroscopic and X-rays studies indicated that the thiosemicarbazone Schiff base and tin atom were coordinated as a parallel five-and six-membered heterocyclic structure. In addition, the bioassay of the synthesized complexes was performed and the results show that the silicon-containing diorganotin complexes with salicylaldehyde thiosemicarbazone have good anticancer activity on human breast cancer cells.