Introduction of a methyl group on the imidazo group (C8-methylimidazole; C8MeI) resulted in enhanced potency (~2×) over C8I against GBM cell lines irrespective of MGMT status (IC50 values ~14 μmol/L and 32 μmol/L in SNB19V and SNB19M cells respectively). The gene discussed is MGMT; the disease is glioblastoma.