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.