Title: Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation
Authors: Lown, J W ×
Krowicki, K
Balzarini, Jan
Newman, R A
De Clercq, Erik #
Issue Date: 18-Nov-1989
Series Title: Journal of Medicinal Chemistry vol:32 issue:10 pages:2368-75
Abstract: A group of oligopeptides have been synthesized which are structurally related to the natural antiviral antitumor antibiotics netropsin and distamycin bearing two such moieties linked by polymethylene bridges. Cytostatic activity against both human and murine tumor cell lines and their in vitro activity against a range of viruses are reported. Enhanced antiviral activity was obtained against vaccinia virus. As a result of the introduction of the polymethylene linkers [( CH2)n, with n = 1, 2, and 6-8], both the antitumor and antivaccinia virus activity was markedly enhanced, relative to that of the parent compounds netropsin and distamycin. The biological activity of these agents is discussed both in terms of their structural differences and in relation to their minor groove binding to duplex DNA.
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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