ALKYLATING AGENT 



Introduction 

Alkylating agents are named because they can add an alkyl group to a molecule.

Alkylating agents can add alkyl groups to molecules in a variety of ways. One common way is through a process called nucleophilic substitution. In nucleophilic substitution, an alkylating agent reacts with a molecule that has a nucleophilic atom, such as a nitrogen atom or an oxygen atom. The nucleophilic atom attacks the alkylating agent, and the alkyl group is transferred to the molecule.

Definition:

An alkylating agent is a substance that causes replacement of hydrogen by an alkyl group especially in a biologically important molecule; specifically : one with mutagenic activity that inhibits cell division and growth and is used to treat some cancers.

Mode of Action of Alkylating Agents: 

  • Alkylating agents are a type of anticancer drugs that work by damaging the DNA of cancer cells and preventing them from replicating. 
  • They have a chemical structure that contains a bifunctional nitrogen mustard moiety which includes two reactive alkyl groups (hence the term alkylation). 
  • The mechanism of action of alkylating agents can be divided into two types: Sn1 and Sn2 reactions.
  • Alkylation is the process of adding an alkyl group (–CH3) to the guanine base of DNA. 
  • This process causes interstrand crosslinking of DNA (formation of covalent bonds between the alkyl group and the DNA base).
  • As a result there is no separation of strands for transcription or Replication. 
  • Cell Death. 


USES - 
  1. Breast cancer
  2. Ovarian cancer
  3. Lung cancer
  4. Leukemia
  5. Lymphoma
  6. Sarcoma

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