A multicomponent condensation between 2-aminobenzimidazole, malononitrile, and an aryl or heteroaryl aldehyde was used for the synthesis of 4-amino-2-aryl-3-cyano-1,2-dihydropyrimido-[1,2-a]benzimidazoles. In addition, a new method of synthesis of the corresponding pyrimido-[2,1-a]benzimidazole derivatives was developed. These syntheses were used to prepare a library of 4-amino-2-aryl-3-cyano-1,2-dihydropyrimido[1,2-a]benzimidazoles and their corresponding pyrimido-[2,1-a]benzimidazole derivatives. This library of compounds was then tested against pancreatic and breast cancer cell lines. A number of compounds were found to possess notable anticancer activity.
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This work was supported by National Institute of General Medical Sciences (P20GM103451) and federal and private funding, including STEM-TRAC, USDA, AREA programs, Florida Blue and Domingo Moreira.
Also the authors wish to thank Prof. Alexander Kornienko, Department of Chemistry and Biochemistry, Texas State University, and Mass Spectrometry Facility, University of New Mexico for mass spectra.
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Published in Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 209-218, February, 2014.
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Risley, V.A., Henry, S., Kosyrikhina, M.V. et al. 4-Amino-2-Aryl-3-Cyano-1,2-Dihydropyrimido-[1,2-a]Benzimidazoles AND their Pyrimidine Analogs as New Anticancer Agents. Chem Heterocycl Comp 50, 185–194 (2014). https://doi.org/10.1007/s10593-014-1460-0
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DOI: https://doi.org/10.1007/s10593-014-1460-0