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Anti-cancer Agents
Anti-cancer Agents
Antimetabolites
Folate antagonists
Folate metabolism- Required for the synthesis of purine nucleotides and thymidylate which are essential for DNA synthesis and cell division. FOLATE--> DHF-->THF--> CH2THF-->CH3THF--> Purine Biosynthesis
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METHOTREXATE- Inhibits the metabolism of folates by inhibiting the action of Dihydrofolate Reductase which converts folate to THF. Maximal effects are S-phase specific (specific to the synthesis phase)
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General MOA: Acts by competition, block or subvert metabolic pathways in the biosynthesis of DNA
Alkylating Agents
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Nitrogen mustards
Derivatives of mustard gas which forms bifunctional DNA adducts. The prodrugs are activated in the liver by Cytochrome P450 enzymes. E.g- CYCLOPHOSPHAMIDE and IFOSFAMIDE
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Cytotoxic Antibiotics
Antracyclines
DOXORUBICIN- Interacts with DNA by intercalation and prevents correct uncoiling and exposure of DNA by stabilising DNA-topoisomerase complex 2. Used to treat leukaemias, lymphomas and solid tumours. Adverse effects: cardiac toxicity
They are flat molecules which interpose themselves between the coils of DNA strands and cause inhibition of macromolecular biosynthesis
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