Cancer is one of the leading causes of death in the current world. Among numerous anticancer drug targets, EGFR is a potential and one of the highly studied drug target. Benzanilide scaffold and its derivatives are the promising groups of compounds with several biological activities including antifungal, antimycotic, antibacterial, spasmolytic, and anticancer. Here, we have tried to develop an improve anticancer compound with benzanilide scaffold. A list of in-silico based benzanilide derivatives was designed and evaluated using molecular docking energy and pharmacophoric interactions in comparison to known EGFR inhibitor. The two optimum compounds A and B were synthesized and tested for their in-vitro anticancer activity by MTT Assay against MCF-7 cell line. Blood lymphocytes were used for studying the effect of the compounds on non-cancerous cells within the human body. The IC₅₀ value of compound A and compound B against MCF-7 was calculated to be 122.3 µM and 101.9 µM respectively. Evaluation of cytotoxic studies of synthesized molecules reveals that both the compounds show cytotoxic activity. The results suggested that compounds A and B could be further explored and studied with more molecular assays to understand its detail activity as an anti-cancer agent.