This Special Issue of Pharmaceuticals presented the recent findings on antiproliferative compounds and highlighted possible routes to discover new drugs used to treat cancer. In this Special Issue, different studies on kinase and methyltransferase-like proteins 3 inhibitors and compounds capable of altering the tumor microenvironment or acting at the mitotic stage of the cell cycle were presented. Furthermore, the antiproliferative or cytotoxic activities of various small synthetic, natural-derived molecules, and their hybrids were discussed.
