Synthesis and Biological Evaluation of 1-(4-(Methylsulfonyl)Phenyl)-5-Phenyl-1H-Pyrazole-4-Carboxamides as Epidermal Growth Factor Receptor-Targeting Anticancer Agents.

We reported the synthesis of novel pyrazole amide derivatives. The newly synthesized compounds are exhibiting in vitro anti-cancer efficacy against MCF-7 and A-549 human cancer cell lines. The compounds, 6m, 6o, and 6p have greater activity against A-549 cell lines with reference to 5-Fluorouracil. Similarly, in vitro, epidermal growth factor receptor results revealed that compounds 6p (50% inhibitory concentration [IC50] = 0.79 ± 0.04 µM) and 6m (IC50 = 0.86 ± 0.06 µM) have shown improved activity in comparison to the standard Erlotinib (IC50 = 0.41 ± 0.03 µM). This article systematically examines the docking studies of lead compounds 6i, 6m, 6o, and 6p, finally found compound 6o showing better binding properties (-10.85 kcal) among all.