A Structure Based, Solid Phase Synthesis Approach to the Development of Novel Selective Estrogen Receptor Modulatory Steroids
Annual rept. 1 Jun 1999-31 May 2000
NORTHEASTERN UNIV BOSTON MA
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The objective of this project is the development of new chemotherapeutic agents for the treatment of hormone responsive breast cancer using a structure-based, solid-phase synthesis approach. We have successfully linked an activated derivative of estradiol to a solid support and converted it to two different series of estrogen receptor ligands. We have begun the biological evaluation of these compounds and initail results suggest that significant receptor affinity is retained. Conformational studies using NMR and computational methods have provided results that can be used in directing the synthesis of newer estrogen receptor binding agents.
- Medicine and Medical Research