Synthesis of pyrimido[1,2-a]benzimidazol-4(10H)-one derivatives and evaluation of their interactions with DNA

The synthesis of new derivatives of the planar tricyclic pyrimido[1,2‐a]benzimidazole system featuring protonable side chains in the 3 and/or 10 positions is described. The reported literature procedures for the preparation of the intermediate 3‐ethoxycarbonylpyrimido[1,2‐a]benzimidazol‐4(10H)‐one 1...

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Bibliographic Details
Published in:Journal of heterocyclic chemistry 2003-11, Vol.40 (6), p.1091-1096
Main Authors: Da Settimo, A., Primofiore, G., Da Settimo, F., Marini, A. M., Taliani, S., Salerno, S., Dalla Via, L.
Format: Article
Language:English
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Summary:The synthesis of new derivatives of the planar tricyclic pyrimido[1,2‐a]benzimidazole system featuring protonable side chains in the 3 and/or 10 positions is described. The reported literature procedures for the preparation of the intermediate 3‐ethoxycarbonylpyrimido[1,2‐a]benzimidazol‐4(10H)‐one 15, starting from 2‐aminobenzimidazole 18 and diethyl ethoxymethylenemalonate, were revised. The interaction with DNA, the intrinsic binding constants, and the antiproliferative activity of a number of compounds (1–8, 10, 11) were preliminarly investigated.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.5570400620