Selective Estrogen Receptor Modulators (SERMs) for the treatment of ER+ breast cancer: An overview

Abstract

Breast cancer is a major threat to women's lives throughout the world. Hormone-dependent or estrogen-receptor positive (ER+) breast cancer accounts for more than 80% of all instances. Selective Estrogen Receptor Modulators (SERMs), which specifically control the ERs and limit the progression of breast malignancy, have drawn the interest of researchers in the treatment of breast cancer by regulation of the estrogen receptors (ER), particularly ERα. The mode of action, anti-proliferative potential, SAR, and favourable interactions of the potent candidates are elaborated. Many potent SERMs with diversity in structural space have been rationally designed and reported in the literature for their anti-breast cancer activity. These SERMs exhibited remarkable anti-proliferative activity against ER+ BC. Since, ERα is responsible for the initiation and progression of BC, there is an urgent need to strategically design and synthesize new SERMs, having more selective binding towards ERα. Long term use of traditionally marketed SERMs is associated with several adverse effects, such as development of endometrial cancer and other disorders. Insight of structural features in the present review will prove to be a guideline for the researchers to design and develop potent SERMs for the treatment of ER+ breast cancer.