Moreover, we describe two novel gefitinib-inspired small molecules, NSC777205 and NSC777207, with wide-spectrum antiproliferative activities and selective cytotoxic preferences for melanoma, renal, central nervous system (CNS), colon, and non-small cell lung cancer (NSCLC) cell lines, and provide in silico mechanistic evidence implicating c-MET/EGFR/phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibition in anticancer activities of these compounds. The gene discussed is PIK3CB; the disease is non-small cell lung carcinoma.