Development of Novel Selective Estrogen Receptor Modulators
Breast cancer is the most common cancer among women worldwide. Estrogen, a sex hormone in women plays a key role in the proliferation of cancer cells especially in post-menopausal women. Selective estrogen receptor modulators (SERMs) like tamoxifen and raloxifene are the most efficient drugs for treatment of breast cancer. These drugs bind to estrogen receptors (ER? or ER? subtypes) in as much as the same manner as estrogen does. However, these drugs are often accompanied by severe side effects. The proposed investigation aims at developing and evaluating new estrogen antagonists. The designed molecules are based on the structure of estrogen itself and are thus expected to show promising bioactivity. We plan to synthesize and bioevaluate a series of rationally designed SERMs, in collaboration of Paraza Pharma Inc. Over the period of 8-months, ~12 rationally designed SERMs will be synthesized, purified and characterized at Acadia University and bioevaluated at Paraza Pharma, Inc.