Abstract
Alkylating agents have been used in the treatment of cancer for over 50 yr, with the nitrogen mustard alkylating agent mechlorethamine being one of the first antitumor drug used in clinical practice half a century ago. These compounds can bind to a variety of cellular structures such as membranes, RNA, proteins, and DNA. It is, however, the ability to form DNA interstrand crosslinks that appears to be the most important event with regard to their antitumor activity. In addition to the nitrogen mustard agents (melphalan, chlorambucil, cyclophosphamide, and ifosfamide), the platinum drugs (cisplatin, carboplatin, and oxaliplatin) have become some of the most widely used cytotoxic anticancer agents.
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