Asseline U, Bonfils E, Dupret D, Thuong N T
Centre de Biophysique Moléculaire, CNRS, Rue Charles Sadron, 45071 Orléans, France.
Bioconjug Chem. 1996 May-Jun;7(3):369-79. doi: 10.1021/bc960024o.
2-Methoxy-6-chloro-9-aminoacridine has been coupled via a polymethylene linker to various positions of an oligonucleotide chain: the 3'-position, using a new universal support, the 5'-position, and both 5'- and 3'-positions via a phosphate. The intercalating agent was also linked to the oligonucleotide chain via an internucleotide phosphorothiolate. The mixture of diastereoisomers was obtained as well as each pure Rp and Sp isomer. Finally, the acridine moiety was introduced to the 5-position of the deoxyuridine. The binding properties of these oligonucleotide-acridine conjugates with their DNA counterparts have been studied by absorption spectroscopy.
2-甲氧基-6-氯-9-氨基吖啶已通过多亚甲基连接体连接到寡核苷酸链的不同位置：使用新型通用载体连接到3'位置，连接到5'位置，以及通过磷酸基团连接到5'和3'位置。嵌入剂还通过核苷酸间硫代磷酸酯连接到寡核苷酸链上。得到了非对映异构体混合物以及每种纯的Rp和Sp异构体。最后，将吖啶部分引入脱氧尿苷的5-位。通过吸收光谱研究了这些寡核苷酸-吖啶缀合物与其DNA对应物的结合特性。
