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

Robert A. Casero; Amy R. Mank; Nada H. Saab; Ronghui Wu; William J. Dyer; Patrick M. Woster

doi:10.1007/BF00685735

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

Robert A. Casero
, Amy R. Mank
, Nada H. Saab
, Ronghui Wu
, William J. Dyer
, Patrick M. Woster

School of Medicine

Research output: Contribution to journal › Article › peer-review

36 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	69-74
Number of pages	6
Journal	Cancer Chemotherapy and Pharmacology
Volume	36
Issue number	1
DOIs	https://doi.org/10.1007/BF00685735
State	Published - Jan 1995

Keywords

CBENSpm
CPENSpm
PENSpm
SSAT activity
mRNA expression

ASJC Scopus subject areas

Oncology
Toxicology
Pharmacology
Cancer Research
Pharmacology (medical)

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10.1007/BF00685735

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title = "Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1",

abstract = "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.",

keywords = "CBENSpm, CPENSpm, PENSpm, SSAT activity, mRNA expression",

author = "Casero, \{Robert A.\} and Mank, \{Amy R.\} and Saab, \{Nada H.\} and Ronghui Wu and Dyer, \{William J.\} and Woster, \{Patrick M.\}",

year = "1995",

month = jan,

doi = "10.1007/BF00685735",

language = "English (US)",

volume = "36",

pages = "69--74",

journal = "Cancer Chemotherapy and Pharmacology",

issn = "0344-5704",

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T1 - Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1

AU - Casero, Robert A.

AU - Mank, Amy R.

AU - Saab, Nada H.

AU - Wu, Ronghui

AU - Dyer, William J.

AU - Woster, Patrick M.

PY - 1995/1

Y1 - 1995/1

N2 - 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.

AB - 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.

KW - CBENSpm

KW - CPENSpm

KW - PENSpm

KW - SSAT activity

KW - mRNA expression

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DO - 10.1007/BF00685735

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SN - 0344-5704

VL - 36

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EP - 74

JO - Cancer Chemotherapy and Pharmacology

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IS - 1

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

Abstract

Keywords

ASJC Scopus subject areas

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