The present invention relates to ENOblock, which is a non-substrate analogue having an enolase inhibitory activity, and a pharmaceutical composition for preventing or treating cancer or enolase-associated diseases, containing the same. The ENOblock of the present invention directly binds to enolase so as to inhibit an activity thereof, and the inhibition is more effective in hypoxia than in normoxia. In addition, the ENOblock of the present invention inhibits migration, metastasis and invasion of cancer cells. Furthermore, the ENOblock of the present invention induces glucose uptake into cells, down-regulates the expression of PEPCK, and inhibits adipogenesis and foam cell formation. Therefore, a composition containing the ENOblock of the present invention can be very effectively applied to prevent or treat cancer or enolase-associated diseases.
