Biological evaluation of amidine derivatives: In vitro cytotoxicity and cellular antioxidant capacity
Year: 2026
Type: article
Abstract: Amidines and related compounds are well known intermediates and protecting groups in organic synthesis. New methodological approaches and obvious structural and functional relevance to guanidines and imidazoles have also prompted interest in the biological activity of these compounds. Here we report a preliminary cytotoxicty evaluation of a set a formamidines and formamidine ureas obtained by convenient and modular synthetic routes. Standard epithelial (Vero, MDCK-SIAT) and fibroblast cell lines (COS-1, COS-7) were employed. All compounds were found to be relatively non-toxic, with LC50 values all in excess of 0.3 mM, but found to vary over the range of compound structures. Cell morphological changes were in good agreement with cell viability. Most of the compounds either suppressed the cellular antioxidant capacity or promoted reactive oxygen species (ROS) generation. The nontoxic nature of these molecules at low to moderate concentrations suggests that the amidine and formamidine urea functional groups are suitable for continued investigation in drug development.
Source: PLoS ONE
Institutions: Universitat Politècnica de Catalunya, Universidad de La Laguna, Pontificia Universidad Católica de Chile, Consejo Nacional de Investigaciones Científicas y Técnicas, Centro Científico Tecnológico - San Luis, National University of San Luis, Barcelona Institute of Science and Technology, Institute for Bioengineering of Catalonia, Georgia Institute of Technology
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $2,382
OpenAlex ID: W7135229659