The concept of click chemistry (CC), first introduced by K.B. Sharpless, has been widely adopted for use in drug discovery, novel drug delivery systems (DDS), polymer chemistry, and material sciences. In this review, we outline novel aspects of CC related to drug discovery and drug delivery, with a brief overview of molecular mechanisms underlying each click reaction commonly used by researchers, and the main patents that paved the way for further diverse medicinal applications. We also describe recent progress in drug discovery and polymeric and carbon material-based drug delivery for potential pharmaceutical applications and advancements based on the CC approach, and discuss some intrinsic limitations of this popular conjugation reaction. The use of CC is likely to significantly advance drug discovery and bioconjugation development.

KB Sharpless首次提出的点击化学（CC）概念已被广泛用于药物发现，新型药物传递系统（DDS），聚合物化学和材料科学中。在这篇综述中，我们概述了与药物发现和药物输送有关的CC的新方面，并简要概述了研究人员常用的每次单击反应背后的分子机制，以及为进一步多样化的医学应用铺平了道路的主要专利。我们还描述了基于CC方法的潜在药物应用和进展中的药物发现以及基于聚合物和碳材料的药物递送的最新进展，并讨论了这种流行的共轭反应的一些固有局限性。CC的使用可能会极大地促进药物发现和生物结合的发展。