Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7426-30. doi: 10.1016/j.bmcl.2011.10.011. Epub 2011 Oct 13.

Abstract

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry
  • Animals
  • Cell Line
  • Dermatitis / prevention & control
  • Diamines / chemical synthesis*
  • Diamines / chemistry
  • Diamines / pharmacology
  • Disease Models, Animal
  • Humans
  • Polyamines / chemistry
  • Radiation-Protective Agents / chemical synthesis*
  • Radiation-Protective Agents / chemistry
  • Rats
  • Reactive Oxygen Species / metabolism
  • Sulfhydryl Compounds / chemical synthesis*
  • Sulfhydryl Compounds / chemistry
  • Sulfhydryl Compounds / pharmacology

Substances

  • 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol
  • Amines
  • Diamines
  • Polyamines
  • Radiation-Protective Agents
  • Reactive Oxygen Species
  • Sulfhydryl Compounds