Synthesis of some 2,4-di- and 2,3,4-trisubstituted benzimidazo[1,2-a] pyrimidines and evaluation of their cytotoxicities towards F2408 and 5RP7 cells

Abstract

This article describes the synthesis of 2,4-di- and 2,3,4-trisubstituted benzimidazo[1,2-a]pyrimidine derivatives which were tested for their cytotoxicities and their spectral characterizations by IR, 1H- and 13C-NMR, EI-MS. The fused title compounds were formed by the reaction of 2-aminobenzimidazole with ß-keto esters or 1,3-alkanediones in PhMe and MeOH or in PPA, respectively, by one-pot cyclocondensation reactions. Complete structural assignments of 2,4-di- and 2,3,4-trisubstituted benzimidazo[1,2-a] pyrimidine derivatives were established by IR, 1H- and 13C-NMR and EI-MS spectroscopic investigations. Single-crystal diffraction analysis was performed for 6. The cytotoxicities of the synthesized compounds on the non-cancer cells (F2408) and cancer cells (5RP7) were evaluated.