<p>Extensive research has been conducted on epigallocatechin and epigallocatechin-3-gallate, common polyphenols found in green tea, focusing on their structural modifications and broad medicinal uses. Chemists specializing in pharmaceuticals have created analogues for epigallocatechin and epigallocatechin-3-gallate, offering multiple therapeutic activities, including anti-cancer, antiviral, antioxidant, low blood sugar, central nervous system, and anti-inflammatory potential. Concurrently, the structure–activity relationship analysis field has steadily increased, leading to the development of numerous derivatives for prospective targets. This paper offers a detailed overview of the biological functions and structure–activity relationship of epigallocatechin and epigallocatechin-3-gallate analogues, aiming to provide a comprehensive review and outlook on epigallocatechin and epigallocatechin-3-gallate analogs.</p> Graphic Abstract <p></p>