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. 2018 Dec 8;19(12):3950. doi: 10.3390/ijms19123950

Table 1.

Chemotherapeutic agents: classification and mechanisms of action.

Mechanism of Action Site of Action Examples
Antimetabolites Interfere with DNA/RNA synthesis by inhibiting purine ring synthesis, ribonucleotide reductase or DNA monomers synthesis normally causing cell death during the S phase of cell growth. Purines and pyrimidines synthesis Thioguanine
Mercaptopurine
Methotrexenate
Ribonucleotides Hydroxycarbamide
DNA monomers Methotrexate
5-Fluorouracil
DNA synthesis Cytarabine
Bleomycin
Intercalating agents Interfere with DNA/RNA synthesis, preventing cell duplication Topoisomerase inhibitors (Etoposide
Topotecan, Irinotecan)
Antibiotics (anthracyclines, Chromomycin, Doxorubicin)
Cross-linking agents Cross-link two DNA bases together preventing DNA from being separated during DNA synthesis or transcription. Nucleotide mispairing, leading to mutations. Alkylating agents
Nitrosoureas
Platinum-based coordination complexes
Enzyme Protein synthesis inhibition, leading to cell death by apoptosis Protein synthesis L-Asparaginase
Microtubule damaging agents Anti-mitotic agents that inhibit cell proliferation by disrupting the normal function of the mitotic spindle. Microtubules Taxanes
Vinca alkaloids
Taxol
Colchicine
Enzyme inhibitors Interfere with normal cell metabolism, leading to cell death Enzyme activity Methotrexate
Kinase inhibitors
Angiogenesis inhibitors Inhibit endothelial cells’ proliferation and tumor growth Angiogenesis Endostatin