Nagatsugi Fumi, Mori Sayaka, Ali Md Monsur, Ogata Yuki, Sasaki Shigeki
Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582 Japan.
Nucleic Acids Symp Ser (Oxf). 2005(49):175-6. doi: 10.1093/nass/49.1.175.
We have previously reported that the oligonucleotides (ODN) containing 2-amino-6-(1-ethylsulfinyl)vinyl purine derivatives (2) exhibit selective and efficient cross-linking to a cytidine at the target site under neutral conditions. In addition, bis-alkylsulfinyl derivative (3b) as the stable precursor of 2 showed the moderate reactivity. In this study, we have searched other bis-alkylsulfinyl precursors to achieve higher cross-linking ability, and found that acetamidoethyl and hydroxyethyl derivatives showed highly efficient and selective reactivity.
我们之前报道过，含有2-氨基-6-(1-乙基亚磺酰基)乙烯基嘌呤衍生物(2)的寡核苷酸(ODN)在中性条件下能在靶位点与胞苷进行选择性高效交联。此外，作为2的稳定前体的双烷基亚磺酰基衍生物(3b)表现出中等反应活性。在本研究中，我们寻找了其他双烷基亚磺酰基前体以获得更高的交联能力，发现乙酰胺基乙基和羟乙基衍生物表现出高效且选择性的反应活性。
