Phytocoumarins, a class of naturally occurring benzopyran-2-ones, exhibit a wide range of biological activities, including antibacterial, anti-inflammatory, antiradical, oncolytic, and monoamine oxidase B (MAO-B) inhibitory effects. These compounds are widely used by researchers to develop novel pharmaceuticals, both natural and synthetic. The study focuses on coumarin hybrids, which are molecularly hybridized compounds designed to exhibit multifunctional pharmacological properties. These hybrids are particularly attractive for treating complex diseases such as cancer, Alzheimer's disease, dysmetabolic syndrome, AIDS, plasmodium infection, and cardiovascular disorders. The authors reviewed 45 relevant papers published between 2004 and 2024 from databases like PubMed, Scopus, Google Scholar, and Web of Science. They aimed to identify and produce highly efficient, tailored coumarin hybrid molecules to aid in the treatment of various human ailments. The study groups these hybrids based on their prospective therapeutic uses and provides recommendations on possible structure–activity relationships.Phytocoumarins, a class of naturally occurring benzopyran-2-ones, exhibit a wide range of biological activities, including antibacterial, anti-inflammatory, antiradical, oncolytic, and monoamine oxidase B (MAO-B) inhibitory effects. These compounds are widely used by researchers to develop novel pharmaceuticals, both natural and synthetic. The study focuses on coumarin hybrids, which are molecularly hybridized compounds designed to exhibit multifunctional pharmacological properties. These hybrids are particularly attractive for treating complex diseases such as cancer, Alzheimer's disease, dysmetabolic syndrome, AIDS, plasmodium infection, and cardiovascular disorders. The authors reviewed 45 relevant papers published between 2004 and 2024 from databases like PubMed, Scopus, Google Scholar, and Web of Science. They aimed to identify and produce highly efficient, tailored coumarin hybrid molecules to aid in the treatment of various human ailments. The study groups these hybrids based on their prospective therapeutic uses and provides recommendations on possible structure–activity relationships.