Synthesis of sex hormone-derived modified steroids possessing antiproliferative activity

During recent years intensive research has been focused on the synthesis of structurally modified steroid hormones in order to obtain compounds with beneficial biological activity such as cell-growth inhibition. Experimental results have revealed that some steroidal derivatives possess direct cytostatic effect on cancer cells in a hormone receptor-independent manner. After a brief account on the most important biological function and characteristics of the naturally occurring sex hormones in physiological and pathological conditions, structural modifications of estrane and androstane scaffolds are discussed in detail. The review covers literature publications (from 2002 to 2012) relating to the synthesis and antiproliferative activity of semisynthetic sex hormone-derived molecules containing simple or heterocyclic substituents. The compounds reviewed are divided into three main categories according to their sterane framework and the nature of substitution. This article is part of a Special Issue entitled "Synthesis and biological testing of steroid derivatives as inhibitors".