Abstract

Estrogens are a group of naturally occurring steroid sex hormones which are characterized by their ability to induce estrus (ovulation) in the female mammal. This article provides a general background and update on the status of steroidal and nonsteroidal estrogens. In addition, the chemistry and clinical applications of steroidal and nonsteroidal antiestrogens, which were developed in recent years, are included. The emphasis on this area has focused on the goal of discovering synthetic antiestrogens devoid of estrogen agonist activity. Representative studies, which have attempted to delineate the mechanism of action for estrogens and antiestrogens, based on binding studies, molecular modeling strategies, or the like, have also been highlighted. An overview of the pharmacology of estrogens is presented with a particular emphasis on receptor-mediated molecular events. Contraception, hormone replacement, and chemotherapy are the three primary therapeutic applications for estrogens. A table listing principal preparations of estrogens for hormone replacement therapy is also included.