María Cristina Caterina, Isabel A. Perillo, Ximena Villalonga, Nicolás Amiano, Cristian Payés, Mercedes L. Sanchez, Alejandra Salerno^*

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Department of Organic Chemistry, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
Faculty of Medicine, University of Buenos Aires, Buenos Aires, Argentina.
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Abstract: A new green synthesis and anti-tumor activity of the series of bis (3-arylimidazolidinyl-1) methanes 1 - 6 are described. The compounds were synthesized from the corresponding N-arylethylenediamine and trioxane as sources of formaldehyde and the reactions were performed in heterogeneous phase catalyzed by an acidic ion-exchange resin (Amberlyst 15). The compounds were tested with the Sulforhodamine B assay according to the protocol of the National Cancer Institute for several cell lines. The results were expressed as percentage inhibition of growth cell in comparison with the full growth of the cells without treatment. Cytotoxicity on normal cells using the Annexing-PI staining and flow cytometry has been evaluated. The parent compound, bis(3-phenylimidazolidinyl-1)methane 1 and the monohalogenated derivatives 4-chlorophenyl 3 and 3-bromophenyl 5 showed antineoplastic activity, 60%, 82% and 89% inhibition growth cell respectively on the human colon cell line (HCT116). The 4-tolyl derivative 6 presented inhibitory activity (73% inhibition of growth cell) on human lung adenocarcinoma cell line (A549) and 62% on human mammary cell line MCF-7.

Keywords: Bis (3-Arylimidazolidinyl-1) Methanes; Amberlyst-15; Anticancer Activity; Cancer Cell Lines; Sulforhodamine B

Cite this paper: M. Caterina, I. Perillo, X. Villalonga, N. Amiano, C. Payés, M. Sanchez and A. Salerno, "New Green Synthesis and Antineoplastic Activity of Bis (3-Arylimidazolidinyl-1) Methanes," Open Journal of Medicinal Chemistry, Vol. 3 No. 4, 2013, pp. 121-127. doi: 10.4236/ojmc.2013.34014.

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