Acquired　immune　deficiency　syndrome　(AIDS)/human　immunodeficiency　virus　(HIV)　is　one　of　the　largest　and　most　devastating　public　health　pandemics　throughout　the　world.　The　global　pandemic　of　drug-sensitive　HIV　and　the　increasing　threat　from　drug-resistant　HIV　result　in　an　urgent　need　to　develop　more　effective　anti-HIV　candidates.　Quinolone　represents　a　significant　class　of　privileged　heterocycles,　and　its　derivatives　possess　promising　in　vitro　and　in　vivo　anti-HIV　properties.　The　4-quinolone　elvitegravir　has　already　been　approved　for　the　treatment　of　HIV;　thus,　quinolone　derivatives　might　be　promising　candidates　with　anti-HIV　activity.　This　review　emphasizes　quinolone　derivatives　with　potential　anti-HIV　activity,　covering　articles　published　between　1992　and　2019.　The　structure-activity　relationship　is　also　discussed　to　provide　insights　for　further　development　of　more　active　quinolone　derivatives.