Title: Synthesis, cytostatic and anti-viral activity evaluation of the novel acyclic nucleoside analogues containing a sterically constrained (Z)-4-amino-2-butenyl moiety
Authors: Wittine, Karlo ×
Benci, Kresimir
Pavelic, Sandra Kraljevic
Pavelic, Kresimir
Bratulic, Sinisa
Hock, Karlo
Balzarini, Jan
Mintas, Mladen #
Issue Date: Apr-2011
Publisher: Birkhäuser Boston
Series Title: Medicinal Chemistry Research vol:20 issue:3 pages:280-286
Abstract: A series of the novel pyrimidine (3-6) and purine (12-15, 18-21) acyclic nucleoside analogues in which the sugar moiety was replaced by a sterically constrained Z-4-amino-, 4-aminohydrochloride-2-butenyl, or aliphatic 4-aminohydrochloride-2-butyl moiety were synthesized and evaluated for their anti-viral and cytostatic activity potency. Cytostatic evaluation of the novel compounds on selected panel of human tumour-cell lines showed that the majority of compounds exerted a non-specific anti-proliferative effect at the highest tested concentration (i.e. 1 x 10(-4) M) against all cell lines. Nevertheless, a rather moderate but selective anti-proliferative effects on HeLa cell cultures in comparison to normal fibroblasts WI 38, were observed for compounds 15 and 21. No anti-viral activity was observed, except for compounds 3, 4, 5 and 19 that showed anti-HIV activity at 50% effective concentration ranging between 10 and 96 mu M.
ISSN: 1054-2523
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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