Synthesis and biological activity of 5-(trifluoromethyl)- and 5-(pentafluorethyl)pyrimidine nucleoside analogues

DOI: 10.1021/jm00358a028

Source and publish data:

Journal of Medicinal Chemistry p. 598 - 601 (1983)

Update date:2022-08-30

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Authors:

Lin Lin

Gao Gao

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Article abstract of DOI:10.1021/jm00358a028

Various 5-substituted perfluoroalkylpyrimidine nucleoside analogues have been synthesized, and their biological activity against L1210, S-180, Vero cells, and herpes simplex virus type 1 (HSV-1) was evaluated. The 5-trifluoromethyl derivatives, 7 and 9, showed significant antiviral activity against HSV-1 with ED₅₀ values of 7 and 5 μM, respectively. In addition, the unblocked nucleoside 9 was found to be about 64-fold less toxic to the host Vero cells and gave a favorable therapeutic index of 64 against HSV-1 in vitro.

Full text of DOI:10.1021/jm00358a028

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