Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity

Bioorg Med Chem Lett. 1998 Mar 17;8(6):635-40. doi: 10.1016/s0960-894x(98)00086-9.

Abstract

A series of N1-monosubstituted putrescine and spermine derivatives was synthesised using a solid phase methodology. We evaluated their cytotoxicity, calmodulin antagonism and polyamine uptake inhibition, pharmacological properties shared by some antitumoral agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amine Oxidase (Copper-Containing)*
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Calmodulin / antagonists & inhibitors
  • Cattle
  • Cell Survival / drug effects
  • Deamination
  • Leukemia L1210 / metabolism
  • Leukemia L1210 / pathology
  • Models, Chemical
  • Oxidation-Reduction
  • Oxidoreductases Acting on CH-NH Group Donors / metabolism
  • Putrescine / analogs & derivatives*
  • Putrescine / pharmacokinetics
  • Spermine / analogs & derivatives*
  • Spermine / pharmacokinetics
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Calmodulin
  • Spermine
  • Amine Oxidase (Copper-Containing)
  • Oxidoreductases Acting on CH-NH Group Donors
  • Putrescine