Synthesis and Biological Evaluations of <i>N</i>-(4-Substituted Phenyl)-7-Hydroxy-4-Methyl-2-Oxoquinoline-1(2<i>H</i>)-Carbothioamides

In continuance of search for new compounds we report herein the expedient and optimized synthesis a series N-(4-substituted phenyl)-7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-carbothioamides (5a-g) in good yields. The anticancer antioxidant activities were determined as per standard protocol. Nearly 5 dozens cancer cell lines derived from nine different panels are used study activity was calculated growth percents (GPs) percent inhibitions (%GIs). molecular docking simulation against one potential targets i.e., epidermal factor receptor (EGFR) done to find putative approach action title 5a-g. N-(4-Nitrophenyl)-7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-carbothioamides (5b) showed most promising with higher sensitivity UO-31, HOP-92, CAKI-1, LOX IMVI T-47D GPs 66.65, 72.63, 85.80, 86.11, 86.96 respectively. compound 5b exhibited an IC50 value 15.21 ± 1.52 µM. efficient binding site EGFR two H-bond interactions residues Gln791 Thr854, π-π stacking π-cationic interaction residue Phe856, while salt bridge Lys745.