Artemisia rupestris L. is one of the therapeutic choices to cure influenza and concomitant infections in China. Rupestonic acid is the main active ingredient of this herbal remedy and has activity against the influenza virus. To find a potential lead compound, more than 300 rupestonic derivatives have been synthesized and assayed in vitro against influenza A and B viruses. This systematic review was therefore aimed at summarizing the rupestonic acid derivatives and their anti-influenza activity studied in the last decade. www.chemistryselect.org