Potential antiradiation drugs containing no nitrogen, and related compounds

Chem Biol Interact. 1986 Feb;57(2):161-74. doi: 10.1016/0009-2797(86)90035-9.

Abstract

Capabilities are reported of di- and higher sulfides (RSnR') terminated by sulfinate functions [-S(O)O-] for protecting mice against otherwise lethal effects of ionizing radiation. With the use of congeners, structure-activity correlations are developed for the effects of esterification of the sulfinate function, of changing the length of the chain of sulfur atoms, of reduction to a mercapto sulfinate, and of changing the substituents R and R' to chiral and other types of groups. Neither a trisulfide nor a sulfinate by itself was significantly radioprotective. The key requirement for radio-protection in the series appears to be the presence of a sulfur function (-Sn-) from which a thiol can be engendered by a neighboring-group effect of an electron-donating group; sulfoxide functions may afford alternatives to sulfinate functions as such neighboring groups. The relevance of structure-activity relations to the chemical and biological mechanisms involved in the radioprotective activities is discussed.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Disulfides
  • Drug Administration Schedule
  • Female
  • Mice
  • Pharmaceutical Vehicles
  • Radiation-Protective Agents* / administration & dosage
  • Structure-Activity Relationship
  • Sulfides*

Substances

  • Disulfides
  • Pharmaceutical Vehicles
  • Radiation-Protective Agents
  • Sulfides