Sulfur and nitrogen-containing heterocycles have received a great deal of attention due to their unique structures and therapeutic relevance. Thiazoles and thiadiazoles are important five-membered heterocycles containing sulfur and nitrogen atoms that draw the special attention of re-searchers due to their synthetic diversity and potent pharmacological properties. Thiazoles and thi-adiazoles are used in agrochemicals, liquid crystals, sensors, the cosmetic industry, cyanine dyes, etc. Sometimes, organic synthesis, including thiazoles and thiadiazoles syntheses with the help of conventional methods, is laborious work, while synthesis of promising organic molecules using microwave irradiation provides better yields, diminishes the reaction time, and reduces unwanted side products. The major causes of death worldwide are due to cancer. Current research demands the design and preparation of novel compounds, including thiazoles and thiadiazoles, that may help to combat cancer, as chemotherapy or chemo drugs suffer from some demerits, including toxicity, lack of selectivity, resistance, and side effects. Hence, the review focuses on the microwave-assisted synthesis of thiazoles and thiadiazoles as a sustainable technique for the first time, and it also aims to highlight the anticancer activities of thiazoles and thiadiazole derivatives elegantly.