DNA alkylators are a class of compounds that can add alkyl groups (e.g., methyl or ethyl groups) to the DNA molecule, leading to DNA damage. This modification can result in mispairing or prevention of DNA replication, which can lead to cell death. Given their ability to damage DNA, alkylating agents are used as chemotherapy drugs to treat various cancers. However, their use can also be associated with significant side effects, as they can damage normal cells in addition to cancer cells. Popular examples of alkylating agents include cyclophosphamide, melphalan, and busulfan.
DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
