Novel class of cyclophosphamide prodrug: cyclophosphamide spiropiperaziniums (CPSP)

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3727-30. doi: 10.1016/j.bmcl.2006.04.049. Epub 2006 May 6.

Abstract

A novel class of cyclophosphamide spiropiperaziniums was synthesized and evaluated for their in vivo anti-cancer activities against S180 and H22. Most of them exhibited definite activities. Especially, compounds 8b and 8k showed good anti-cancer activities, meanwhile, 8k also showed much lower toxicity than CP. Several interesting structure-activity relationships were revealed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cyclophosphamide / analogs & derivatives
  • Cyclophosphamide / chemical synthesis*
  • Cyclophosphamide / pharmacology*
  • Inhibitory Concentration 50
  • Mice
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology*
  • Prodrugs
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Piperazines
  • Prodrugs
  • Spiro Compounds
  • Cyclophosphamide