Antineoplastic agent Mechanism of action











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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. • #AmitLunkad

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