In vitro Antitumour Activity, Genotoxicity, and Antiproliferative Effects of Aminophosphonic Acid Diesters and their Synthetic Precursors

Abstract

The Schiff bases N-furfurylidene-p-toluidine and N-(4-dimethylaminobenzilidene)-p-toluidine, and the recently synthesized aminophosphonic acid diestersthylaminophenyl)]toluidine were tested for in vitro antitumour activity on six human epithelial cancer cell lines. The genotoxicity and antiproliferative activity of these compounds were tested in mice. The aminophosphonates showed high in vitro antitumour activity towards the breast cancer-derived cell lines (MCF-7 and MDA-MB-231), the cervical carcinoma cell line (HeLa), and the human colon adenocarcinoma cell line (HT-29). In addition, the Schiff base N-furfurylidene-p-toluidine signifi cantly inhibited the growth of bladder carcinoma cells (647-V) and the hepatocellular carcinoma line HepG2, and U-shaped dose-response curves were observed after treatment of 647-V and MCF-7 cells. All studied compounds had a moderate genotoxic and antiproliferative activity in vivo.

Synthesis, characterization and toxicity studies of pyridinecarboxaldehydes and L-tryptophan derived Schiff bases and corresponding copper (II) complexes

“…Again, HeLa cells were more susceptible to the cytotoxicity of Cu-4pyr.Trp than KCL-22 cells ( Figure 5, B ). Earlier, several Schiff bases were tested in vitro for their cytotoxic activity against different cell lines and the structure activity relationship of compounds was discussed 17 , 31 , 32 . Furthermore, Kril et al .…”

In vitro biological and in silico screening of novel iron(iii) complexes for DNA-targeted antitumor drug component

“…The absorbance (Abs) of each sample was measured at 570 nm using a microplate reader (Epoch, BioTek). 40–44 The formula is % viability = (Abs E /Abs C ) × 100, where Abs E is for the mean absorbance value of the experimental group and the Abs C is for the mean absorbance value of the control group. 45,46 The half-maximal inhibitory concentration (IC 50 ) values were calculated depending on the regression equation in the graphic.…”