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

✍ Scribed by A. Da Settimo; G. Primofiore; F. Da Settimo; A. M. Marini; S. Taliani; S. Salerno; L. Dalla Via

Publisher
Journal of Heterocyclic Chemistry
Year
2003
Tongue
English
Weight
64 KB
Volume
40
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

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(10__H__)‐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.

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