Radiomimetic alkylating agents

Cradiom, A.R. and J.J. Roberts. 1965. Reactions of cultured mammalian cells of varying radiosensitivity widi die radiomimetic alkylating agent mustard gas.. Prog. Biochem. Pharmacol. 1 320-326. 

Table 6. Effect of thiosulphate and cysteine on LD50 of nitrogen mustards. Reproduced from the paper by Connors, T.A., Jeny, A and Jones, M. (1964), Reduction of the toxicity of radiomimetic alkylating agents in rats by thiol pretreatment-III. The mechanism of the protective action of thiosulphate. Biochem. Pharmacol., 13, 1545-1550... 

DNA s5mthesis and also interfere with cell replication. Alkylating agents has got cytotoxic action and damage the nuclei of growing and multiplying cells. They have got immunosuppressant action also and suppress antibody production. They also have radiomimetic (like ionizing radiation) actions. 

Mustard is an alkylating agent similar to drugs that have been used in cancer chemotherapy, such as nitrogen mustards, Cytoxan, and cis-platin. Since DNA is one of mustard s most sensitive targets, it is not surprising that carcinogenesis and radiomimetic effects are seen. ... 

Thiotepa is an alkylating agent, which is a cell-cycle nonspecific alkylating agent related to nitrogen mustard. Its radiomimetic action is believed to occur through the release of ethylenimine radicals, which disrupt the bonds of DNA. TEPA possesses cytotoxic activity. 

---