Izvestiya of Saratov University.

Chemistry. Biology. Ecology

ISSN 1816-9775 (Print)
ISSN 2541-8971 (Online)


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

Autors: 
Ivonin Maksim Andreevich, Saratov State University
Fomin Alexander S., Institute of Biochemistry and Physiology of Plants and Microorganisms of the Russian Academy of Sciences
Burygin Gennady L., Institute of Biochemistry and Physiology of Plants and Microorganisms of the Russian Academy of Sciences
Sorokin Vitaly Viktorovich, Saratov State University
Abstract: 

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 ?g/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 ?g/ml, respectively. For 5-phenyl-1,2,3,4,5,6-hexahydrobenz[4,5] imidazolo[1,2-a]quinazoline, the IC50 value was 100 ?g/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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Received: 
27.07.2019
Accepted: 
13.10.2019
Published: 
20.11.2019