Radioprotective drugs

Thiirane is more bactericidal than oxirane, and derivatives of 2-mei captomethylthiirane inhibit tuberculosis. The following pharmacological uses have been reported for compounds derived from thiirane derivatives gold complexes of the adducts of diethylphosphine and thiirane (antiarthritic), adducts of thiiranes and malononitrile (antibacterial, blood vessel dilators, muscle relaxants, sedatives), thermolysis products of thiirane 1-oxides and adducts of thiirane 1-oxides with sulfenyl chlorides (antibacterial), adducts of 2,3-diarylthiirene 1,1-dioxides with ynamines (antibacterial, parasiticidal), adducts of 2,3-diarylthiirene 1,1-dioxides with enamines (antifertility), adducts of p-aminophenylacetic esters with thiirane (immunosuppressants), adducts of amines and thiiranes (radioprotective drugs). 

Ohta, S., N. Sakurai, T. Inoue and M. Shinoda. Studieson chemical protectors against radiation. XXV. Radioprotective activities of various crude drugs. Yakugaku Zasshi 1987 107(1) 70-75. 

Substitution at some positions of psoralene reduce the activity, which decreases as the chain becomes longer (the 3-methyl derivative is not very active).76 Some compounds, such as 5,9-dihydroxypsoralene,77 are used as radiosensitizing drugs, and trioxasalene (2,5,9-trimethylpsora-lene) is used as a radioprotective.300- 13... 

Drug delivery -for radioprotective agents [RADIOPROTECTIVE AGENTS] (Vol 20)... 

Smoluk GD, Fahey RC, Calabro-Jones PM, Aguilera JA, Ward JF (1988a) Radioprotection of cells in culture by WR-2721 and derivatives form of the drug responsible for protection. Cancer Res 48 3641-3647... 

The 1,3-dioxolane ring is found in a major antifungal drug, ketoconazole (123). Ketoconazole is a broad spectrum, orally active antifungal agent and is used to treat a wide variety of superficial or deep fungal infections. Various workers, especially in Russia, have explored the use of simple oxathiolanes as radioprotectants. For example, the survival rate of mice irradiated with lethal doses of X- or -y-rays was 40% when they were pretreated with 2,2-dimethyl-l,3-oxathiolane. Other oxathiolanes were less active. 1,3-Oxathiolane, administered intravenously to dogs 2 or 3 times daily for 2-4 days before chronic irradiation with polonium-210, increased their life expectancy from 9 months to 3-7 years and alleviated radiation sickness. Some blood indicators were also restored to normal. 

Advances include radioprotective drugs applied during radiotherapy of neoplastic diseases. Effects similar to the enzyme superoxide dismutase have been found in copper complexes of Schiffs bases (derived from different amino acids and salicylaldehyde). Activity of complexes is dependent on their structures. The structural changes of their chelate rings are responsible for their effects on free radicals produced in organisms during radiation. Complexes have square pyramidal pentacoordination, which is similar to the coordination polyhedron in the active center of the Cu-dependent superoxide dismutase. The complexes used as radio-protective drugs play an important role in radiotherapy. They protect healthy tissues and cells from injurious radiation. ° ... 

It must be higher than 1.3 for clinical use and ideally higher than 2 for management of a nuclear accident. Of course, an ideal radioprotector will have to demonstrate other characteristics compatibility with other drugs, effectiveness for various types of radiation, low cost, possible synthesis in large quantity, stability... The aim of this work was to study the incorporation of potentially radioprotective organic compounds in organometallic... 

Rima G., Satge J., Dagiral R., Lion C., Fatome M., Roman V, Laval J.D., Synthesis and radioprotective activity of new organosilicon and germanium compounds, Metal-Based Drugs, 1998, 5, 139-146. 

Snyder, J.E., Hamid, Q., Wang, C., Chang, R., Emami, K., Wu, H., Sun, W., 2011. Bioprinting ceU-laden matrigel for radioprotection study of liver by pro-drug conversion in a dual-tissue microfluidic chip. Biofabrication 3, 034112. 

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