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Antiestrogens can be defined as compounds that prevent the stimulation of transcription by the estrogen receptor complexes. Two main types of antiestrogens are known: nonsteroidal estrogen receptor antagonists (often designed as “selective estrogen receptor modulators,” SERMs) and pure estrogen receptor antagonists. Anti-Estrogen

Nonsteroidal antiestrogens interfere with the transcription process by binding to the hormone recognition site in the estrogen receptor and preventing the induction of the conformational change necessary to recognition of the co-activators. However, due to the fact that estrogen receptors of different target tissues vary in chemical structure, they may show mixed biological responses, behaving as antagonists in one tissue and as agonists in another.

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The pure antiestrogens are analogs of the natural hormones that bear long, flexible side chains at C-7. In contrast to SERMs, these compounds bind to the estrogen receptor preventing its dimerization and binding to DNA, probably because their side chains bind to the receptor outside the steroid-binding region.

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