The steroid sulfatase (STS) plays a major role in the regulation of steroid hormone concentrations in several human tissues and target organs and therefore, represents an interesting target to regulate estrogen and androgen levels implicated in different diseases. In this review article, the emphasis is put on STS inhibitors reported in the fruitful 2000-2010 decade, which consolidated the first ones that were previously developed (1990-1999). The inhibitors reviewed are divided into four categories according to the fact that they are sulfamoylated or not or that they have a steroid nucleus or not. Other topics such as function, localization, structure and mechanism as well as applications of STS inhibitors are also briefly discussed to complement the information on this crucial steroidogenic enzyme and its inhibitors.