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Published on: January 19, 2015
Synthesis and anti-HIV activity of 4'-modified cyclopentenyl pyrimidine C-nucleosides
1BK21-Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
Abstract:
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).
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