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Synthesis 2006(14): 2305-2312
DOI: 10.1055/s-2006-942444
DOI: 10.1055/s-2006-942444
PAPER
© Georg Thieme Verlag Stuttgart · New York
Synthesis and Characterization of Some Novel 2-(Trifluoromethyl)pyrimido[1,2-a]benzimidazoles and Pyrimido[1,2-a]benzimidazol-2H)-ones of Biological Interest
Further Information
Received
24 February 2006
Publication Date:
28 June 2006 (online)
Publication History
Publication Date:
28 June 2006 (online)
Abstract
The synthesis of some potentially active 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazoles and pyrimido[1,2-a]benzimidazol-2(1H)-ones by the cyclization of 4-alkoxyvinyl trifluoro(chloro)methyl ketones with 2-aminobenzimidazole is described. The structure of the products was assigned based on 1H and 13C NMR as well as 2D-NMR experiments. Some of the obtained products exhibited significant DNA-topoisomerase I inhibitory activity.
Key words
2-aminobenzimidazole - pyrimidobenzimidazole - enones - halogenated heterocycles - DNA-topoisomerase I inhibitory activity
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