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

摘要

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-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.

主权项

1. A method for protecting a subject from ionizing radiation, the method comprising:
administering systemically to a subject in need thereof an amount of a radioprotector compound comprising a free thiol and a positively-charged backbone, the radioprotector compound comprising a structure according to:wherein R and R′ are independently selected from H, CH3, alkyl, and heteroalkyl;
wherein the amount is effective to protect the subject from ionizing radiation; wherein systemic administration of the radioprotector compound to the subject is accomplished by intraperitoneal injection or intravenous injection.