Specific modification of nucleic acids inside the cell with alkylating derivatives of oligonucleotides ethylated at internucleotide phosphates

Knorre, D.G.; Zarytova, V.F.; Karpova, G.G.; Stephanovich, L.E.

Nucleic Acids Symposium Series 9: 195-198


ISSN/ISBN: 0261-3166
PMID: 6117830
Document Number: 180911
The alkylating derivatives of (C6H5NH)2P[dTp(Et)]4U and [dTp(Et)]9 U with completely esterified internucleotide phosphates bearing reactive 2,3 -O-4(N-2-chloroethyl N-methylamino)-benazylidene moiety attached to 3 -end cis-diol group were prepared. These alkylating derivatives of non-ionisable oligonucleotide analogs were demonstrated to penetrate efficiently into Krebs ascites tumor cells and to alkylate nucleic acids inside the cells with a strong preference towards complementary poly(A)-fragments of mRNA.

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