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Chemical Structure and Classification The main compounds that have demonstrated a pure antiestrogenic activity in the laboratory are the following (Fig. 6.1) 1. ICI 164384. This is the first pure antiestrogen discovered (Wakeling and Bowler 1987). This compound is a 7a-alkylamine derivative of 17 ft-estradiol, with a 16-atom carbon chain in the 7a position. 2. Fulvestrant. Also called ICI 182780 and Faslodex, this compound is also a 7a-alkylamine derivative of 17 -estradiol, developed from ICI...

Mechanism of Action in the Endometrium

As has been widely commented in previous chapters, the agonist antagonist profile of a given SERM is determined by the type of compound and the particular target tissue. Members of the different SERM families bind to the ligand-binding domain (LBD) of the ER, whose particular crystal structure has been revealed for estradiol and for raloxifene (Brzozowski et al. 1997). Once inserted into the binding cavity, estradiol makes direct hydrogen bonds bewteen its A-ring and the carboxylate of Glu 353,...