Lee Jae Young, Oh Chang Hyun, Ko Ok Hyun, Hong Joon Hee
College of Pharmacy, Chosun University, Kwangju 501-759, South Korea.
Nucleosides Nucleotides Nucleic Acids. 2002 Oct;21(10):709-21. doi: 10.1081/NCN-120015727.
A series of novel acyclic nucleosides 10, 11, 21, and 22 were synthesized efficiently starting from D-lactose. The condensation of the mesylate 5 and 16 with an adenine and cytosine base under standard nucleophilic substitution conditions (K2CO3, 18-Crown-6, DMF) afforded a series of acyclic novel nucleosides. Compound 21 displayed moderate anti-HCMV activity in the AD-169 cells (EC50 = 18.5 microg/mL) without exhibiting any cytotoxicity up to 100 microM.
从D-乳糖开始，高效合成了一系列新型无环核苷10、11、21和22。在标准亲核取代条件下（碳酸钾、18-冠-6、N,N-二甲基甲酰胺），甲磺酸酯5和16与腺嘌呤和胞嘧啶碱基缩合，得到了一系列新型无环核苷。化合物21在AD-169细胞中表现出中等的抗人巨细胞病毒活性（半数有效浓度=18.5微克/毫升），在高达100微摩尔的浓度下未表现出任何细胞毒性。
