Background: Styrylquinolines are characteristic fully aromatic compounds with flat,
rather lipophilic structures. The first reports on their synthesis and biological activity were published
roughly a century ago. However, their low selectivity, unfavorable toxicity and problems
with their mechanism of action significantly hampered their development. As a result, they have
been abandoned for most of the time since they were discovered.
Objective: Their renaissance was observed by the antiretroviral activity of several styrylquinoline
derivatives that have been reported to be HIV integrase inhibitors. Subsequently, other activities
such as their antifungal and anticancer abilities have also been revisited.
Methods: In the present review, the spectrum of the activity of styrylquinolines and their use in
drug design is presented and analyzed.
Results: New properties and applications that were reported recently have re-established
styrylquinolines within medicinal and material chemistry. The considerable increase in the number
of published papers regarding their activity spectrum will ensure further discoveries in the field.
Conclusion: Styrylquinolines have earned a much stronger position in medicinal chemistry due to
the discovery of their new activities, profound mechanisms of action and as drug candidates in