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Presence of a substantial amount of receptor alpha (ERα) in a breast cancer sample is an index of favorable response to tamoxifen and related antiestrogens.Unfortunately, a significant proportion of such ERα-positive tumors manifest de novo or acquired resistance to these agents, stressing the importance of producing new drugs able to antagonize ERα action.The search for compounds aimed at interfering with the recruitment of co-regulators involved in ERα-mediated transcription has been recently initiated in various laboratories.Drugs able to impede the interaction of the LxxLL consensus motif (NR box) of such co-activators with the activation function 2 (AF-2) localized within the hormone binding domain (HBD) of the receptor have been synthesized.