SYNTHESIS AND ANTI-HIV PROPERTY OF NOVEL OLIGO-DNA PHOSPHOROTHIOATE ANALOGS BEARING AN INTERCALATIVE MOIETY AND OR POLYAMINE RESIDUES/

Novel oligoDNA phosphorothioate analogs (S-ODN-1 to -3) bearing an int ercalative moiety at the 5'-terminus and/or polyamine at the C-5 posit ion of certain uridine residues substituting for normal thymidine resi dues were synthesized and their physicochemical properties as well as the anti-HIV activities were studied. The analogs have identical base sequence which is complementary to art/tris region of human immunodefi ciency virus type 1 (HIV-1). The polyamine moiety on the analogs is fo und to be effective not only to enhance the hybridization ability but also reduce the non-specific cytotoxicity and strengthen the anti-HIV activity of the analogs.