An inhibitor of Gal-1; decreases lactose binding to Gal-1 (Kds = 290 and 100 μM in the presence and absence of compound, respectively); cytotoxic against a cancer cell panel with IC50 values that directly correlate to Gal-1 mRNA expression; inhibits proliferation of HUVECs (IC50 = 2 μM) and reduces HUVEC migration in a wound healing assay; reduces tumor growth in the MA148 ovarian mouse xenograft model and the B16 murine melanoma syngeneic model via decreases in tumor microvessel density and induction of apoptosis (2.4 and 10 mg/kg)