Breast cancer is the most common type of cancer in women worldwide and it is the second cause of cancer death after lung cancer. There have been many efforts in producing various pharmaceuticals for breast cancer treatment and among them Nanopharmaceutical Sciences have been extremely of high importance. All the drugs used to treat a cancer were usually shown unpleasant side effects. Chlorambucil is an older antineoplastic (anticancer) drug that is an alkylating agent with many known side

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... s for the patients. Recent findings have shown that the uptake of polyamine compounds such as amino acids (e.g. Methionine) in cancer cells is mostly increased. In this study a molecular antineoplastic conjugate, Chlorambucil-Methionine was developed and evaluated on the breast cancer MCF-7 cell line. For evaluation MTT assay, apoptosis assay and necrosis assay were employed but the mechanism of cell death or toxicity comparison were investigated by apoptosis-necrosis assay or abnormal toxicity test. Chlorambucil-Methionine as a targeted antineoplastic conjugate has shown higher antineoplastic properties and had not shown abnormal toxicity. The conjugate showed very good anticancer effects same as Chlorambucil but it had less toxicity in comparison with Chlorambucil. Apoptosis was the mechanism for most cell death in this study. Based on the results Chlorambucil-Methionine conjugate may be a better option than Chlorambucil alone for the treatment of breast cancer. Further study is recommended to confirm these findings in clinical practice.