Combi-nitrosourea molecule 27 (Figure 15), releasing a DNA cross-linking agent and an inhibitor of MGMT, was designed in response to cancer resistance to chloroethylnitrosoureas (CENUs) induced by MGMT, which repairs O6-alkylated guanine and, subsequently, inhibits the formation of dG–dC cross-links. The gene discussed is MGMT; the disease is cancer.