Oxasteroids and their derivatives are a class of bioactive molecules derived from the modification or alteration of steroid structures. These compounds exhibit diverse biological activities, making them valuable in pharmaceutical research. Oxasteroids typically feature an oxygen atom at the C1 position of the steroid ring system, creating unique structural features that can influence their pharmacological properties. They have been explored for their potential therapeutic applications in areas such as anti-inflammatory, antiviral, and anticancer treatments. Structurally, oxasteroids can be modified through various chemical reactions to introduce functional groups like hydroxyls, ethers, or ketones, enhancing their specificity and effectiveness. These derivatives often exhibit improved solubility, better tissue distribution, or altered metabolic stability compared to their parent compounds. The synthesis of oxasteroids involves complex organic reactions, including ring-opening epoxidations, alkylation, and esterification. Due to their structural diversity and biological versatility, oxasteroids and their derivatives are promising candidates for the development of novel therapeutic agents in drug discovery processes.