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

  • Original Article
  • PENSpm, CBENSpm, CPENSpm, SSAT Activity, mRNA Expression
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Abstract

Three unsymmetrically substituted polyamine analogues demonstrate significant and selective antitumor effects. Each of the analoguesN 1-ethyl-N 11-propargyl-4,8-diazaundecane (PENSpm),N 1-ethyl-N 11-(cyclobutyl)methyl-4,8-diazaundecane (CBENSpm), andN 1-ethyl-N 11-(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/spermineN 1-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.

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Authors and Affiliations

  1. Oncology Center, Johns Hopkins University School of Medicine, 424 North Bond Street, 21231, Baltimore, MD, USA

    Robert A. Casero Jr., Amy R. Mank & William J. Dyer

  2. Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Profession, Wayne State University, 48202, Detroit, MI, USA

    Nada H. Saab, Ronghui Wu & Patrick M. Woster

Authors
  1. Robert A. Casero Jr.
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  2. Amy R. Mank
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  3. Nada H. Saab
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  4. Ronghui Wu
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  5. William J. Dyer
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  6. Patrick M. Woster
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Casero, R.A., Mank, A.R., Saab, N.H. et al. Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1. Cancer Chemother. Pharmacol. 36, 69–74 (1995). https://doi.org/10.1007/BF00685735

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  • DOI: https://doi.org/10.1007/BF00685735

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