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Synthesis and anti-HCMV activity of novel acyclic nucleosides
Jae Young Lee1, Chang Hyun Oh, Ok Hyun Ko
1College of Pharmacy, Chosun University, Kwangju 501-759, South Korea.
Nucleosides, Nucleotides & Nucleic Acids
|December 28, 2002
Abstract:
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.