Liu Lian Jin, Hong Joon Hee
BK21-Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
Nucleosides Nucleotides Nucleic Acids. 2009 Apr;28(4):303-14. doi: 10.1080/15257770902946058.
Novel syntheses of 4'-modified cyclopentenyl pyrimidine C-nucleosides were performed via C-C bond formation using S(N)2 alkylation via the key intermediate mesylates 6 and 16, which were prepared from acyclic ketone derivatives. When antiviral evaluation of synthesized compound was performed against various viruses such as HIV-1, HSV-1 and HSV-2, isocytidine analogue 20 showed moderate anti-HIV activity in CEM cell line (EC(50) = 13.1 micromol).
通过使用关键中间体甲磺酸酯6和16进行S(N)2烷基化形成C-C键，实现了4'-修饰的环戊烯基嘧啶C-核苷的新型合成，甲磺酸酯6和16由无环酮衍生物制备。当对合成化合物针对多种病毒（如HIV-1、HSV-1和HSV-2）进行抗病毒评估时，异胞苷类似物20在CEM细胞系中显示出中等的抗HIV活性（EC(50)=13.1微摩尔）。
