Title: Synthesis and cytotoxic activity of 6-vinyl- and 6-ethynyluridine and 8-vinyl-and 8-ethynyladenosine
Authors: Manfredini, S ×
Baraldi, P G
Bazzanini, R
Marangoni, M
Simoni, D
Balzarini, Jan
De Clercq, Erik #
Issue Date: 19-Feb-1995
Series Title: Journal of Medicinal Chemistry vol:38 issue:1 pages:199-203
Abstract: It is well-known that the introduction of vinyl and ethynyl moieties into nucleosides is of crucial importance for cytostatic, antiviral, or other biological activities. In this study 6- and 8-vinyl-and -ethynyluridine and -adenosine were prepared by a general procedure involving the palladium-catalyzed cross-coupling of trimethylsilylacetylene or vinyltributyltin. The introduction of a vinyl group at C-6 of uridine or an ethynyl group at C-8 of adenosine resulted in nucleoside derivatives showing cytostatic activity against several murine and/or human tumor cell lines. Interestingly, 8-vinyladenosine had pronounced selective inhibitory effects on human (Molt/4F and MT-4) versus murine (L1210 and FM3A) tumor cell lines.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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