Chrysin is a naturally occurring flavonoid, mainly found in honey, propolis and in many plant species. Owing to its multiple pharmacological properties such as antioxidant, anti-inflammatory, anti-allergic, anti-diabetic, antiestrogenic, antibacterial, neuroprotective activity and antitumor activities, chrysin has become the foremost candidate among flavonoids in recent years. Chrysin derivatives had also seen potential applications in anticancer drug delivery. Due to issues such as bioavailability and absorption associated with Chrysin, its therapeutic benefits remained nascent unlike other flavonoids. To overcome these limitations and to obtain compounds with improved efficacy and developing more active drugs efforts had been made by designing analogs and conjugates of Chrysin. The target of the current review is to articulate the recent progress in research on synthesis and pharmacological activities of Chrysin derivatives. Additional information on the basic chemical reactivity of Chrysin, its bioavailability and toxicity is also presented in this article.