Flexible estrogen receptor modulators

Abstract

Tamoxifen is a selective estrogen receptor modulator (SERM) with a triarylethylene structure, which has estrogenic activity in bone and endometrial tissue, yet antagonises the actions of estrogen in other tissues including breast tissue. It was proposed in the present work to develop novel diaryl and triaryl analogues with a preferable, more selective activity profile than that of tamoxifen. This thesis is presented in three different sections. The first section covers the synthesis of a number of novel, flexible and non-fiexible analogues closely related to the anti-estrogen tamoxifen. The second section includes the synthesis of dihydrochalcones and subsequently, from these, the preparation of numerous highly flexible tamoxifen analogues. The structures of these products were verified using the following; TLC analysis, melting points, 1H NMR, 13C NMR, F19 NMR, and Infra-red spectrometry and Mass spectrometry.