In recent eras, cancer, and tuberculosis have become the leading causes of not only morbidity but also mortality. Around 10 million cancer-related fatalities are reported annually worldwide, but 10.4 million new cases are also discovered each year. According to World Health Organization data, 10.4 million cases were in 2016 worldwide, whereas 360,565 cases in Indonesia was reported. Some clinically approved anticancer and anti-TB drugs demonstrate a most promising role in their treatment. Still, the need for new, powerful, and secure candidates as anticancer and Anti TB agents with a variety of modes of action is constantly present due to the serious growth of drug resistance, side effects, multidrug-resistant malignancies, and tuberculosis as a result of mutations. Over the last decade, various heterocyclic compounds in medicinal chemistry were explored and reported frequently in the literature; these derivatives have received substantial attention as anticancer and anti-TB agents. In which nitrogen-containing heterocyclic moiety, isatin emerged as a significant and versatile heterocyclic for developing novel anticancer and anti-TB candidates.