TITLE:
New Green Synthesis and Antineoplastic Activity of Bis (3-Arylimidazolidinyl-1) Methanes
AUTHORS:
María Cristina Caterina, Isabel A. Perillo, Ximena Villalonga, Nicolás Amiano, Cristian Payés, Mercedes L. Sanchez, Alejandra Salerno
KEYWORDS:
Bis (3-Arylimidazolidinyl-1) Methanes; Amberlyst-15; Anticancer Activity; Cancer Cell Lines; Sulforhodamine B
JOURNAL NAME:
Open Journal of Medicinal Chemistry,
Vol.3 No.4,
December
4,
2013
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.