Indolin-2-one is a pharmacologically beneficial scaffold with several biological features. The role of oxindole may be recognized to be varied by various chemical groups to provide novel biological activities as a chemical scaffold for creating and developing biologically active drugs. Cancer treatment has advanced significantly in recent years. The oxindole multitarget kinase inhibitor sunitinib, which is taken orally, inhibits specific receptor tyrosine kinases. Sunitinib has shown potential anticancer impact in phase II trials of individuals with diverse cancers, including hepatocellular carcinoma, pancreatic neuroendocrine tumors, and renal cell carcinoma. The most frequent adverse effects of sunitinib, pharmacokinetic/pharmacodynamic studies, drug-drug interactions, and mechanism of action of sunitinib are also discussed. The review focuses on resistance developed in almost all responding patients, a significant cause of therapy failure. More studies are needed to investigate the mechanisms of antiangiogenic agent resistance to discover new analogs capable of circumventing antiangiogenic agent resistance with better therapeutic properties.