Application | 2-chloro-5-iodopyrazine can be used to prepare tetra-substituted olefin compounds with the following structure. This type of compound is a covalent antagonist of estrogen receptor. This class of compounds can be used to inhibit the growth of MCF7ER-α (wild type) and MCF7ER-α(Y537S mutant) cells. Other compounds known to inhibit the growth of cell cultures of MCF7ER-α (wild type) cells, such as tamoxifen, raloxifene (raloxifene) and fulvestrant, are currently used to treat breast cancer in human patients. Therefore, the compounds disclosed herein can be used to treat breast cancer in human patients expressing ER-α, and can be used to treat breast cancer in human patients expressing Y537S mutant ER-α. |