Synthesis, antiviral and antiproliferative activity of a new class of 5-(alkyl or arylthio)-6-vinyl uracils.
Uracil derivatives bearing substituted or unsubstituted vinyl groups at position C6 and alkyl- or arylthio groups at position C5 were synthesized and tested in vitro for antiviral and antiproliferative activity. None of the compounds were active against HIV-1. However, some of them inhibited the proliferation of leukemia, lymphoma and solid tumor-derived cell lines at micromolar concentrations. The maximum potency of antiproliferative activity correlates with the presence of unsubstituted vinyl groups and alkyl- or arylthio substituents.
Baraldi
P G
PG
Cacciari
B
B
Romagnoli
R
R
Spalluto
G
G
Garuti
L
L
Roberti
M
M
Pani
A
A
Perra
G
G
Scintu
F
F
Pinna
N
N
Musiu
C
C
La Colla
P
P
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D013873:Thionucleotides / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014753:Vinyl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D013873:Thionucleotides; D014753:Vinyl Compounds; D014498:Uracil