Table 4.
Representative samples of hypoxia responsive prodrug.
| Type | Agent | Reduction | Mechanism of action |
|---|---|---|---|
| Nitro(hetero)cyclic compounds | Evofosfmide (TH-302) | 1e− | DNA alkylation |
| PR-104 | 1e−/2e− | DNA interstrand cross-links | |
| Etanidazole | 1e− | DNA alkylation | |
| Misonidazole | 1e− | DNA alkylation | |
| Quinones | Apaziquone (EO9) | 1e−/2e− | DNA alkylation |
| quinone mitomycin C (MMC) | 1e−/2e− | DNA interstrand cross-links | |
| Porfiromycin | 1e− | DNA interstrand cross-links | |
| Indolequinone | 1e− | DNA alkylation | |
| Aromatic N-oxides | Tirapazamine (TPZ) | 1e− | Topoisomerase ll poisoning and DNA doublestrand breaks |
| SN30000 | 1e− | Complex DNA damage | |
| QdNOs | 2e− | Reduce hypoxic gene expression | |
| Aliphatic N-oxides | Banoxantrone (AQ4N) | 2e− | DNA binding and Topoisomerase II inhibition |
| OCT 1002 | 2e− | DNA binding and Topoisomerase II inhibition | |
| Transition metals complexes | Pt(IV) | 2e− | DNA binding |
| Au(I) | 2e− | ROS generation | |
| Cu(II) | 2e− | ROS generation |