Novel CoA-polyamine conjugates for effective inhibition of spermine/spermidine-N1-acetyltransferase

New mimics of the transition state of spermine/spermidine-N(1)-acetyltransferase reaction were prepared starting from aminooxy analogues of spermidine or spermine and SH-CoA. The activity depended on the structure of polyamine fragment of the conjugate and best of the synthesized compounds were acti...

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Bibliographic Details
Published in:Nucleosides, nucleotides & nucleic acids nucleotides & nucleic acids, 2007, Vol.26 (10-12), p.1245-1248
Main Authors: Simonian, Alina, Khomutov, Alex, Hyvonen, Tapani, Grigorenko, Nikolay, Keinanen, Tuomo, Vepsalainen, Jouko, Alhonen, Leena, Janne, Juhani
Format: Article
Language:English
Subjects:
Acetyltransferases - antagonists & inhibitors
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Coenzyme A - chemistry
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Molecular Mimicry
Spermidine - analogs & derivatives
Spermine - analogs & derivatives
Structure-Activity Relationship
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Summary:New mimics of the transition state of spermine/spermidine-N(1)-acetyltransferase reaction were prepared starting from aminooxy analogues of spermidine or spermine and SH-CoA. The activity depended on the structure of polyamine fragment of the conjugate and best of the synthesized compounds were active at micromolar concentrations.
ISSN:1525-7770
1532-2335
DOI:10.1080/15257770701528214