Covalent organic frameworks (COFs) are a multipurpose substance that has obtained many notices for cancer treatment because of their multiple features, such as minimal cytotoxicity, adjustable pores, outstanding crystal structure, simple modification/functionalization, and excellent adaptability. To acquire a better understanding of COFs synthesis and its significance in biomedical contexts, a comprehensive review of their properties and applications is presented below. Initially, an overview of the diverse chemical linkages used in creating a range of bonds in COFs is provided, along with a categorization of various synthesis techniques. Next, the article delves into the biomedical uses of COFs, emphasizing their role as carriers for transporting various substances and applications in cancer treatment, biosensors, bioimaging, and sterilization processes. Finally, potential opportunities and current obstacles are discussed to extend the practical utility of COFs afterward. Overall, the advancement of COFs is in its early stages, yet their distinctive properties have laid a strong foundation for their potential use in disease diagnosis and treatment. C1 [Moharramnejad, Mojtaba; Karimi, Farideh; Mirtamizdoust, Babak; Ehsani, Ali] Univ Qom, Fac Sci, Dept Chem, Qom, Iran. [Moharramnejad, Mojtaba] Univ Qom, Young Researcher & Elite Grp, Qom, Iran. [Sayah, Taraneh; Ghehsareh, Zahra] Univ Isfahan, Dept Chem, Esfahan 81746, Iran. [Rezaei, Mahsa Mohammad] Univ Guilan, Fac Sci, Dept Chem, Guilan, Iran. [Amini, Ali Hossein] Golrang Ind Grp GIG, Golrang Pharmaceut Investment Co GPI, Soroush Mana Pharmed, Tehran, Iran. [Malekshah, Rahime Eshaghi; Shahi, Mehrnaz] Semnan Univ, Dept Chem, Semnan, Iran. [Haribabu, Jebiti] Univ Atacama, Fac Med, Carreras 1579, Copiapo 1532502, Chile. [Haribabu, Jebiti] Chennai Inst Technol, Chennai 600069, India. [Hsu, Sodio C. N.] Kaohsiung Med Univ Hosp, Dept Med Res, Kaohsiung 80708, Taiwan. [Hsu, Sodio C. N.] Kaohsiung Med Univ, Dept Med & Appl Chem, Kaohsiung 80708, Taiwan. C3 University of Qom; University of Qom; University of Isfahan; University of Guilan; Semnan University; Universidad de Atacama; Chennai Institute of Technology; Kaohsiung Medical University; Kaohsiung Medical University Hospital; Kaohsiung Medical University