Antineoplastic agent: Mechanism of action

Alkylating agents contain chemical groups that can form covalent bonds with particular nucleophilic substances in the cell
• Produce highly reactive carbonium ion intermediates
• Forms covalent bond with electron donors like amine, hydroxyl and sulfhydryl groups
• Alkylating agents are bifunctional, i.e. they have two alkylating groups
• The nitrogen at position 7 (N7) of guanine, being strongly nucleophilic, is probably the main molecular target for alkylation in DNA
• N1 and N3 of adenine and N3 of cytosine may also be affected
• Being bifunctional they can cause intra- or interchain cross-linking, abnormal base pairing or chain scission
• Interferes not only with transcription but also with replication
Main impact is seen during replication (S phase) when some zones of the DNA are unpaired and more susceptible to alkylation.
• Results in a block at G2 and subsequent apoptotic cell death.
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[@nabeelakhan3760]

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[@Pharmacy43]

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Thank you...

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Thanks

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