Chemical nuclease is a new challenging field that is quickly developing in chemical biology. Metal complex of macrocyclic polyamines can hydrolyze DNA and RNA, the ability depends on metal ions and their side groups conjugated to them. In this dissertation, we focus on creating new chemical nucleases through incorporation of cyclen into peptides. Through the coupling of cyclen and homoserine deriva-tive, we have firstly synthesized a cyclen-functionalized ?α-amino acid, (S)-2-amino-4[1 (1, 4, 7, 10 –tetraazacyclo-dodecane)] butanoic acid. Subsequently, coupling the amino acid and other natural amino acid by using DCC, nine dipeptides have been obtained. Preliminary studies on the cleavage of DNA in the presence of metal complexes have also been performed in this dissertation. The results showed that the Zn(Ⅱ) complexes of cyclen-fuctionalized dipeptides didn't cleave DNA obviously, but their Cu(Ⅱ) complexes can do this cleavage reaction very well.
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