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Lysineenediyne conjugates as photochemically triggered DNA double-strand cleavage agents{
 

Summary: Lysine­enediyne conjugates as photochemically triggered DNA double-
strand cleavage agents{
Serguei V. Kovalenko and Igor V. Alabugin*
Received (in Cambridge, UK) 10th November 2004, Accepted 23rd December 2004
First published as an Advance Article on the web 25th January 2005
DOI: 10.1039/b417012a
Statistical analysis of DNA-photocleavage by two types of
lysine­enediyne conjugates confirms that more double-strand
breaks are produced than can be accounted for by coincident
single-strand breaks.
In recent years, considerable effort has been invested into
development of synthetic reagents that selectively cleave DNA
under irradiation with visible or UV light without the use of metals
or reducing agents.1
The ability of these chemical systems to
generate reactive organic intermediates on demand represents a
promising approach to new antitumor therapeutic strategies.
Enediyne antibiotics are among the most potent natural
anticancer agents. Their biological activity stems from cyclization
of the enediyne moiety to a reactive p-benzyne diradical followed

  

Source: Alabugin, Igor - Department of Chemistry and Biochemistry, Florida State University

 

Collections: Chemistry; Biology and Medicine