Dimethyl (2-Furyl)-N-(2-Methoxyphenyl)Aminomethylphosphonate Induces Apoptosis in Esophageal Squamous Cancer Cells. Structure Versus Activity of its Selected Analogs

Abstract

Cytotoxicities of several new aminophosphonic compounds bearing 2-furyl moiety 2b-d and 3a-c on KYSE 30, 150, and 270 esophageal cancer cell lines are reported here. The qualitative study on correlations between the structure and cytotoxic activity of furan-deriving aminophosphonates has been performed. Dimethyl (2-furyl)-N-(2-methoxyphenyl)aminomethylphosphonate (2a), which has been previously shown to have the interesting values of cytotoxicity on these esophageal cancer cell lines was tested and found to induce apoptosis. The analyses of correlations between apoptosis, necrosis, and viability were also performed.

Relationship between Structure and Antibacterial Activity of α-Aminophosphonate Derivatives Obtained via Lipase-Catalyzed Kabachnik−Fields Reaction

“…The distinctive character of bioactive organophosphorus compounds has established their wide applicability in agricultural and medicinal chemistry [ 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 ]. α-Aminophosphonates ( Figure 1 ) play a crucial role as a platform to design new drugs [ 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 ]. Among other advantages, there are several reports regarding their antimicrobial activity; alafosfalin, for example, a simple dialkyl α-aminophosphonate, exhibits activity against pathogenic E. coli , S. aureus , Bacillus , and K. pneumonia strains ( Figure 1 ) [ 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 ].…”