Development of novel alkylating agent against glioblastoma (GBM) led to the discovery of selective, non-toxic for the healthy cells and potent anti-glioblastoma drug candidate. The compound showed a significant cytotoxic effect against glioblastoma cancer cells and in mice model of the diseases. To date, only one chemotherapic drug, temozolomide, TMZ (a DNA alkylator) has been approved for the specific treatment of GBM, in combination with surgery and radiotherapy. The biggest problematic issue with TMZ treatment is that cancer cells very quickly become resistant to the drug. We hope that the proposed project will serve as a starting point for the development of a novel and effective anti-glioblastoma therapy.