Name Mode of Action References
(±)Amethopterin (Methotrexate) Blocks thymidine biosynthesis via inhibition of dihydrofolate reductase (folic acid antagonist) [42]
3Amino1,2,4benzotriazine
1,4dioxide
Hypoxia activated antineoplastic agent [43]
Aminopterin Mechanism same as methotrexate but more potent. [44]
Cytosine- β D-arabinofuranoside Selective inhibitor of DNA synthesis. [45]
5-Fluoro5' deoxyuridine Inhibits proliferation of cancer cells transformed by HRas or Trk oncogenes [46]
5-Fluorouracil Depletes dTTP and inhibits thymidylate synthetase; it forms nucleotides that can be incorporated into RNA and DNA and induces p53dependent apoptosis [47]
Ganciclovir In suicide gene therapy of solid tumors, the gene for Herpes
simplex virus thymidine kinase is delivered to tumor cells and expressed, which in turn activates ganciclovir cytotoxicity.
[48]
Hydroxyurea Blocks the synthesis of deoxynucleotides by inactivating ribonucleoside reductase resulting into inhibition of DNA synthesis and induction cell death. [49]
Mitomycin C Inhibits DNA synthesis, nuclear division, and proliferation of cancer cells. [50]
Table 3: DNA synthesis inhibitors and their mode of action as anticancer agent.