960化工网
Synthesis and triplex forming properties of pyrrolidino pseudoisocytidine containing oligodeoxynucleotides
Alain Mayer,Adrian Häberli,Christian J. Leumann
Organic & Biomolecular Chemistry Pub Date : 04/07/2005 00:00:00 , DOI:10.1039/B502799C
Abstract

Pyrrolidino pseudo-C-nucleosides are isosteres of natural deoxynucleosides which are protonated at the pyrrolidino ring nitrogen under physiological conditions. As constituents of a triplex forming oligodeoxynucleotide (TFO), the positive charge is expected to stabilise DNA triple helices via electrostatic interactions with the phosphodiester backbone of the target DNA. We describe the synthesis of the pyrrolidino isocytidine pseudonucleoside and the corresponding phosphoramidite building block and its incorporation into TFOs. Such TFOs show substantially increased DNA affinity compared to unmodified oligodeoxynucleotides. The increase in affinity is shown to be due to the positive charge at the pyrrolidino subunit.

Graphical abstract: Synthesis and triplex forming properties of pyrrolidino pseudoisocytidine containing oligodeoxynucleotides
平台客服
平台客服
平台在线客服