Ultrasmall MoS2 nanocrystals have unique optoelectronic and catalytic properties that have acquired significant attraction in many areas. We propose here a simple and economical method for synthesizing the luminescent nanocrystals MoS2 using the hydrothermal technique. In addition, the synthesized MoS2 nanocrystals display photoluminescence that is tunable according to size. MoS2 nanocrystals have many advantages, such as stable dispersion, low toxicity and luminescent characteristics, offering their encouraging applicability in biomedical disciplines. In this study, human lung cancer epithelial cells (A549) are used to assess fluorescence imaging of MoS2 nanocrystals. MTT assay, trypan blue assay, flow cytometry and fluorescence imaging results have shown that MoS2 nanocrystals can selectively target and destroy lung cancer cells, especially drug-resistant cells (A549).