Summary
Thiazolidinyl- and perhydrothiazinyl-ethyl-N-mustard-phosphamide esters were designed to act as highly specific suicide inactivators of DNA polymerase α holoenzymes. Acute and subacute toxicity of these drugs in mice was very small. By daly i. p. injection, on day 0–4 mice were cured of P388 lymphatic leukaemia with no depression of blood leucocytes. The findings suggest that suicide inactivators of DNA polymerase α holoenzyme may be promising drugs for low toxicity cancer chemotherapy.
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Supported by Bundesministerium für Forschung und Technologie, Bonn-Bad Godesberg
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Hohorst, HJ., Bielicki, L., Müller, K. et al. Low toxicity cancer chemotherapy by suicide inactivation of DNA polymerase α holoenzyme: first results with new thiazolidinyl-and perhydrothiazinyl-ethyl-N-mustard-phosphamide esters. J Cancer Res Clin Oncol 114, 309–311 (1988). https://doi.org/10.1007/BF00405840
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DOI: https://doi.org/10.1007/BF00405840