Title: Novel DNA groove binding alkylators: design, synthesis, and biological evaluation
Authors: Krowicki, K ×
Balzarini, Jan
De Clercq, Erik
Newman, R A
Lown, J W #
Issue Date: 18-Mar-1988
Series Title: Journal of Medicinal Chemistry vol:31 issue:2 pages:341-5
Abstract: A group of oligopeptides has been synthesized that are structurally related to the natural antiviral antitumor agents netropsin and distamycin but which bear alkylating functions. Cytostatic activity against both human and murine tumor cell lines as well as their in vitro activity against a range of viruses is reported. The biological activity of these agents is discussed both in terms of their alkylating reactivity and of their structural differences. The incorporation of alkylating moieties into these minor groove DNA binders results in up to 45-fold increase in cytostatic activity compared with netropsin and up to 18 times the activity of distamycin.
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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