Current status on development of steroids as anticancer agents

A complete update on various steroids used as anticancer agents. Steroidal antiproliferative (antihormones and antiestrogens) and cytotoxic (naturally occurring, modified and steroid conjugates) lead molecules have been described. •A complete update of steroidal anticancer leads of last 25 years.•Various antihormonal (antiproliferative and enzyme inhibitor agents) approaches through steroid molecules have been included.•Naturally occurring, semisynthetic and E2 conjugates have been discussed. Steroids are important biodynamic agents. Their affinities for various nuclear receptors have been an interesting feature to utilize them for drug development particularly for receptor mediated diseases. Steroid biochemistry and its crucial role in human physiology, has attained importance among the researchers. Recent years have seen an extensive focus on modification of steroids. The rational modifications of perhydrocyclopentanophenanthrene nucleus of steroids have yielded several important anticancer lead molecules. Exemestane, SR16157, fulvestrant and 2-methoxyestradiol are some of the successful leads emerged on steroidal pharmacophores. The present review is an update on some of the steroidal leads obtained during past 25 years. Various steroid based enzyme inhibitors, antiestrogens, cytotoxic conjugates and steroidal cytotoxic molecules of natural as well as synthetic origin have been highlighted. This article is part of a Special Issue entitled “Synthesis and biological testing of steroid derivatives as inhibitors”.