The linear naphtho-γ-pyrone (LNGP) moiety is a naturally occurring scaffold with broad biological activity ranging through antimicrobial, antiviral, insecticidal and anti-estrogenic activity. This review, the first of its kind, surveys the chemical literature in an effort directed toward assembling data that will facilitate the construction of activity profiles associated with this emerging class of compounds. The structural and associated biological information has been presented in tabular format with all structures revealed throughout the document and referencing that will allow the reader to rapidly access the literature pertaining to a specific activity or structural class.