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Ivonin M. A., Fomin A. S., Burygin G. L., Sorokin V. V. Comparison of Cytotoxic Activity of Compounds from the Benzimidazolequinazoline and Pyridopyrimidine Series. Izvestiya of Saratov University. Chemistry. Biology. Ecology, 2019, vol. 19, iss. 4, pp. 396-400. DOI:

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Comparison of Cytotoxic Activity of Compounds from the Benzimidazolequinazoline and Pyridopyrimidine Series


Colorimetrically using the MTT assay the cytotoxic activity of 5-aryl-1,2,3,4,5,6-hexahydrobenz[4,5]imidazolo[1,2-a]quinazolines and a tautomeric mixture of 4-amino-2-phenyl-6H-pyrido[1,2-a] pyrimidin-3-carbonitrile with 2-(phenyl(pyridin-2-ylamino)methyl)- malononitrile was screened. These compounds were obtained by the three-component condensation of aromatic aldehydes (benzaldehyde, 3-bromobenzaldehyde, 4-methoxybenzaldehyde), heterocyclic amines (2-aminobenzimidazole or 2-aminopyridine) and cyclohexanone or malonic acid dinitrile in comparison with the starting amines. Compounds were tested at concentrations of 100, 50, 25, 12.5, 6.25, 3.12, and 1.61 μg/ml on monolayer cell lines of the African green monkey kidney (Vero). IC50 values for the most active compounds (5-(4-methoxyphenyl)-1,2,3,4,5,6- hexahydrobenz[4,5]imidazolo[1,2-a]quinazoline and a tautomeric mixture of 4-amino-2-aryl-6H-pyrido[1,2-a]pyrimidine-3-carbonitrile with 2-(phenyl(pyridin-2-ylamino)methyl)-malononitrile were 75 and 50 μg/ml, respectively. For 5-phenyl-1,2,3,4,5,6-hexahydrobenz[4,5] imidazolo[1,2-a]quinazoline, the IC50 value was 100 μg/ml. For the remaining compounds, IC50 was not detected, and the starting 2-aminobenzimidazole and 2-aminopyridine inhibited the metabolic activity by only 20–30% at maximum concentrations. The values of the half-inhibitory concentration determined using the MTT assay are similar to the values, which were obtained earlier in the cytotoxic studies of similar heterocyclic compounds by AlamarBlue assay.

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