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An alkylating agent is a compound that substitutes an alkyl group, Cn H 2n+1, for an active hydrogen atom in an organic compound, with DNA as the principal target.
Alkylating agents were developed from mustard gas in 1946. Reaction with DNA, RNA or proteins leads to alkylation, which may be bifunctional and cause DNA crosslinking
Commonly used alkylating agents include busulphan, melphalan, cyclophosphamide, chlorambucil, thiotepa, ifosfamide and mustine (nitrogen mustard).