A Structure Based, Solid Phase Synthesis Approach to the Development of Novel Selective Estrogen Receptor Modulatory Steroids

Abstract

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.

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Document Details

Document Type
Technical Report
Publication Date
Jun 01, 2000
Accession Number
ADA383168

Entities

People

  • Robert Hanson

Organizations

  • Northeastern University

Tags

Communities of Interest

  • Biomedical

DTIC Thesaurus Topics

  • Alkenes
  • Chemical Synthesis
  • Chemistry
  • Computational Science
  • Drug Abuse
  • Electronic Mail
  • Health Services
  • Hormones
  • Organic Chemistry
  • Phase
  • Radioactive Decay
  • Radiotherapy
  • Regression Analysis
  • Solid Phases
  • Two Dimensional

Fields of Study

  • Chemistry

Readers

  • Molecular Biology and Genetics
  • Organic Chemistry
  • Systems Analysis and Design