U. Berghoff et al., MONOFUNCTIONAL TRANS-PT-II(NH3)(2) MODIFICATION OF PYRIMIDINE-RICH DEOXYOLIGONUCLEOTIDES - DIRECT PLATINATION AND USE OF A PROTECTIVE GROUP, Inorganica Chimica Acta, 269(1), 1998, pp. 135-142
Ways are studied to obtain pyrimidine-rich deoxyoligonucleotides (ON)
(n = 4-8) which are monofunctionally modified with a trans-[Pt(NH3)(2)
Cl](+) entity: (i) direct platination of the ON with trans-Pt(NH3)(2)C
l-2; (ii) platination with the monoaqua species trans-[Pt(NH3)(2)Cl(H2
O)](+); (iii) platination with trans-Pt(NH3)(2)(1-MeT)Cl or trans-[Pt(
NH3)(2)(1-MeT)(H2O)](+) containing the acid-labile protective group 1-
MeT (1-MeT = 1-methylthymine anion). Reactions with the oligonucleotid
es are followed by H-1 NMR spectroscopy and HPLC and the products are
characterized by ESI MS and H-1 NMR. It was the aim of this work to fi
nd ways of preparing monofunctionally (trans-Pt-II(NH3)(2)) modified O
N on a large scale for potential application in the antisense technolo
gy. (C) 1998 Elsevier Science S.A.