Registration Number
0213U002333,
0112U003750
, R & D reports
Title
Design, synthesis and biological testing of new heterocyclic inhibitors of topoisomerase I as potential antitumoral agents
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Head
Dubey Igor, Доктор хімічних наук
Registration Date
23-01-2013
Organization
Institute of Molecular Biology and Genetics of NASU
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The series of new heterocyclic compounds of several classes, derivatives of benzimidazole, phenazine, quinoline, cyanines etc., were obtained. Their biological activity was studied in vitro in the enzymatic system of pTZ19R plasmid DNA relaxation by topoisomerase I E.coli. Aryl-substituted benzimidazole derivatives reveal inhibitory effect on the enzyme at 50-100 uM concentration. Cyanine derivatives are highly active topoisomerase inhibitors: a number of compounds quantitatively suppress enzyme activity at 2-10 uM concentration, and for the most active cyanine the IC90 value is equal to 1 uM. It was shown that cyanines efficiently bind to DNA forming stable complexes that determines their biological activity. For the other compounds this binding was found to be weak or absent. Inhibition activity of benzimidazole derivative CL5 may be based on its binding to topoisomerase.
Product Description
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Ільченко М.М.
Дубей Л.В.
Костенко О.М.
Криворотенко Д.В.
Кузів Я.Б.
Негруцька В.В.
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2020-04-02
