Britannica Sources used in this answer

How do alkylating agents and antimetabolites attack cancer cells?

Created from Britannica articles using AI. AI can make mistakes, so verify using Britannica articles.

Alkylating agents and antimetabolites are types of anticancer drugs that function as cytotoxic agents, primarily targeting rapidly dividing cells.1

Alkylating Agents

These highly reactive drugs bind to chemical groups in DNA and RNA, causing structural damage that prevents nucleic acid replication. Key mechanisms include:2
* Cross-linking: Creating bonds between strands of DNA.2
* DNA Breakage: Inducing breaks in the nucleic acid or causing the loss of basic components like purines.2
By damaging DNA, these agents prevent cancer cells from reproducing, ultimately leading to cell death.21

Antimetabolites

These substances are structurally similar to normal cellular metabolites or enzymatic substrates. They attack cancer cells by:3
* Mimicry: Competing with or replacing natural metabolites required for DNA and RNA synthesis.31
* Enzyme Inhibition: Being incorporated into nucleic acids or inhibiting enzymes, which disrupts normal metabolic functioning and prevents the synthesis of new genetic material.3

Because these drugs interfere with essential cellular processes, they are particularly toxic to rapidly growing and dividing cells.31