Synthesis and properties of oligonucleotides carrying cryptolepine derivatives
1Department of Structural Biology, Instituto de Biología Molecular de Barcelona, C.S.I.C., Jordi Girona 18-26, E-08034 Barcelona. recgma@cid.csic.es
Abstract:
A carboxy derivative of the antimalarial cytotoxic drug cryptolepine was introduced into synthetic oligonucleotides by reaction of the carboxy derivative of cryptolepine with oligonucleotides carrying an amino group either at the 3'- or at the 5'-end. Oligonucleotides carrying the cryptolepine derivative bind their complementary sequences with greater affinity than unmodified ones. When cryptolepine is attached to a polypyrimidine oligonucleotide designed to form a parallel triplex, the triplex shows none or weak stabilization.
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