The aim of this study was to develop a novel nanosize drug candidate for cancer therapy. For this purpose, (S)-methyl 2-[(7-hydroxy-2-oxo-4-phenyl-2H-chromen-8yl)methyleneamino]-3-(1H-indol-3-yl)propanoate (ND3) was synthesized by the condensation reaction of 8-formyl-7-hydroxy-4-phenylcoumarin with L-tryptophan methyl ester. Its controlled release formulation was prepared and characterized by different spectroscopic and imaging methods. The cytotoxic effects of ND3 and its controlled release formulation were evaluated against MCF-7 and A549 cancer cell lines, and it was found that both of them have a toxic effect on cancer cells. For drug design and process development, the molecular docking analysis technique helps to clarify the effects of some DNA-targeted anticancer drugs to determine the interaction mechanisms of these drugs on DNA in a shorter time and at a lower cost. By using the molecular docking analysis and DNA binding assays, the interaction between the synthesized compound and DNA was elucidated and non-binding interactions were also determined. To predict the pharmacokinetics, and thereby accelerate drug discovery, the absorption, distribution, metabolism, excretion and toxicity values of the synthesized compound were determined by in silico methods.
Electrochemical determination of paracetamol (PC) using an electrode prepared by a one step electropolymerization of the new coumarin-based Schiff base-doped PEDOT conductive polymer on a highly oriented pyrolytic graphite (HOPG) substrate is reported. The electrodes were characterized by Fourier transform infrared spectroscopy, scanning electron microscopy, and X-ray diffraction analysis. The possible interference effects of ascorbic acid, uric acid, dopamine, glucose, and caffeine were investigated by chronoamperometry in the presence of paracetamol. The sensor (PEDOT-MC1/HOPG-10 Scan) has a high sensitivity to paracetamol, with a limit of detection (LOD) of 0.312 µM and a RSD % of 1.22 (S/N = 3). In addition, real sample analyzes were performed on pharmaceutical samples for PC determination using the prepared sensor (PEDOT-MC1/HOPG-10 Scan).
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