Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1

Cancer Chemother Pharmacol. 1995;36(1):69-74. doi: 10.1007/BF00685735.


Three unsymmetrically substituted polyamine analogues demonstrate significant and selective antitumor effects. Each of the analogues N1-ethyl-N11-propargyl-4,8-diazaundecane (PENSpm), N1-ethyl-N11-(cyclobutyl)methyl-4,8-diazaundecane (CBENSpm), and N1-ethyl-N11-(cyclopropyl)methyl-4,8-diazaundecane (CPENSpm) is cytotoxic to a representative non-small-cell lung carcinoma line, NCI H157, while being only growth-inhibitory to a representative small-cell-lung carcinoma line, NCI H82. Cytotoxicity is accompanied by a significant increase in expression of the polyamine catabolic enzyme spermidine/spermine N1-acetyltransferase (SSAT) at the levels of activity and steady-state mRNA. These new analogues are significant both for their cell-type-specific activity and as synthetic prototypes for the addition of SSAT-activated functional groups.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetyltransferases / metabolism
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Dose-Response Relationship, Drug
  • Humans
  • Lung Neoplasms / drug therapy*
  • Ornithine Decarboxylase / metabolism
  • Polyamines / therapeutic use*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured / drug effects


  • Antineoplastic Agents
  • N(1)-ethyl-N(11)-(cyclobutyl)methyl-4,8-diazaundecane-1,11-diamine
  • Polyamines
  • Acetyltransferases
  • diamine N-acetyltransferase
  • Ornithine Decarboxylase