Synthesis and Analysis of Novel Tamoxifen Derivatives

Indianapolis, IN

Breast cancer is the most common cancer among women and is the second leading cause of cancer-related death. It is primarily treated using hormone therapy, if applicable, in conjunction with surgery and radiation. Of the current hormone therapies, Tamoxifen is currently widely used for estrogen receptor positive breast cancer. Tamoxifen acts as an antiestrogen, preventing binding of estradiol to estrogen receptor. Though Tamoxifen is effective in preventing proliferation of breast cancer cells, it has significant drawbacks that call for improvements. The goal of this research is to develop novel derivatives with similar biological activity that may not have the adverse side effects. Two compounds have been synthesized and tested using a binding assay and a cell activity assay to determine potential efficacy in breast cancer as an antiestrogen. These compounds have been shown to bind with moderate affinity and act as antiestrogens in breast cancer cells.