人类越来越严峻的未满足医疗需求和对抗各种疾病的持续斗争通过研究产生了新的分子。随着疾病的演变，不同的策略被采用来对抗新的挑战，发现更安全、更有效和特异性更强的治疗药物。在几种新颖的方法中，生物连接是一种简单方便的技术，合成更有活性的分子。类固醇系统已被广泛用作药物发现和开发过程中具有显著多元化药物特性的特权骨架。类固醇分子因其刚性和良好穿透生物膜的能力而备受青睐。对基本环结构进行轻微改变将导致生成具有广泛治疗活性的类固醇衍生物。类固醇不仅本身具有活性，而且与各种生物活性基团结合可以增加它们的亲脂性、稳定性和靶向特异性，并降低不良反应。因此，类固醇核心明显表现为小分子的生物载体。类固醇生物连接物具有多种优点，如与较低剂量的协同活性以及选择性疗法等，减少了不良反应。类固醇生物连接物已被广泛研究，用于治疗各种疾病，并显示出作为抗癌、抗炎、抗凝血、抗微生物、杀虫剂/农药、抗氧化和抗病毒剂以及其他几种杂散活动的显著效用。本文全面回顾了类固醇生物连接物作为药物活性分子的治疗进展。本综述涵盖了类固醇生物连接物潜在的生物应用，并将有益于更广泛的科学界在药物开发中的努力。© 2022 The Authors. Published by American Chemical Society.

Ever increasing unmet medical requirements of the human race and the continuous fight for survival against variety of diseases give birth to novel molecules through research. As diseases evolve, different strategies are employed to counter the new challenges and to discover safer, more effective, and target-specific therapeutic agents. Among several novel approaches, bioconjugation, in which two chemical moieties are joined together to achieve noticeable results, has emerged as a simple and convenient technique for a medicinal chemist to obtain potent molecules. The steroid system has been extensively used as a privileged scaffold gifted with significantly diversified medicinal properties in the drug discovery and development process. Steroidal molecules are preferred for their rigidness and good ability to penetrate biological membranes. Slight alteration in the basic ring structure results in the formation of steroidal derivatives with a wide range of therapeutic activities. Steroids are not only active as such, conjugating them with various biologically active moieties results in increased lipophilicity, stability, and target specificity with decreased adverse effects. Thus, the steroid nucleus prominently behaves as a biological carrier for small molecules. The steroid bioconjugates offer several advantages such as synergistic activity with fewer side effects due to reduced dose and selective therapy. The steroidal bioconjugates have been widely explored for their usefulness against various disorders and have shown significant utility as anticancer, anti-inflammatory, anticoagulant, antimicrobial, insecticidal/pesticidal, antioxidant, and antiviral agents along with several other miscellaneous activities. This work provides a comprehensive review on the therapeutic progression of steroidal bioconjugates as medicinally active molecules. The review covers potential biological applications of steroidal bioconjugates and would benefit the wider scientific community in their drug discovery endeavors.© 2022 The Authors. Published by American Chemical Society.