Derivatives of the MO-I-1100 inhibitor, second-generation MO-I-1151 (with a trifluoromethyl group substitution instead of chlorine) 14, and third-generation MO-I-1182 (in which the trifluoromethyl group was replaced with a carboxymethyl group) 15, efficiently enhanced the potency of ASPH inhibition in in vitro assays of tumor cell proliferation, migration, and invasion. The gene discussed is ASPH; the disease is neoplasm.