In the field of medicinal chemistry, thiazole, a heterocycle containing sulfur and nitrogen atoms, plays a significant role. It is a key core scaffold found in numerous naturally occurring (e.g. vitamin B1 or thiamine) and synthesized compounds that exhibit significant medicinal value. The 1,3-thiazole scaffold is the mainstay of numerous clinically used drugs, such as nizatidine, meloxicam, ritonavir, tiazofurin, bleomycin, and nitazoxanide. Molecules containing thiazole nuclei are attractive targets in medicinal chemistry attributed to their broad spectrum of biological functions, such as antiproliferative, antioxidant, antitubercular, anti-inflammatory, and antimicrobial activities. This chapter discusses the different synthesis pathways of thiazole-embodying molecules and their anticancer, antitubercular, antioxidant, and antimicrobial activities, reflecting upon numerous biological applications.