Solid-Phase Combinatorial Approach to Estradiol Tamoxifen/Raloxifene Hybrids: Novel Chemotherapeutic/Prophylactic Selective Estrogen Receptor Modulators (SERM)

Abstract

The objective of this project is the development of new chemotherapeutic agents for the treatment of hormone-responsive breast cancer using a solid phase approach to synthesize new agents having features common to both steroids and antiestrogens. During the past year we have functionalized the carboxy resin with both the E-and Z-tributylstannylvinyl estradiol. We have prepared and characterized the initial series of iodophenoxyalkylamines that will be coupled to the resin-bound steroid. The biological assays have been established and validated using series of previously prepared compounds. Molecular modeling and NMR spectrometric methods for conformational analyses and for data analysis have been developed. The next years specific aims involve the synthesis and evaluation of the initial series of target compounds.

Open PDF

Document Details

Document Type
Technical Report
Publication Date
Jul 01, 2001
Accession Number
ADA399600

Entities

People

  • Robert N. Hanson

Organizations

  • Northeastern University

Tags

Communities of Interest

  • Biomedical

DTIC Thesaurus Topics

  • Alkenes
  • Assays
  • Bioassay
  • Breast Cancer
  • Chemical Compounds
  • Chemical Shifts
  • Chemical Synthesis
  • Chemistry
  • Chemotherapeutic Agents
  • Computational Science
  • Data Analysis
  • Health Services
  • Hormone Antagonists
  • Regression Analysis
  • Solid Phases
  • Statistical Analysis
  • Two Dimensional

Fields of Study

  • Chemistry

Readers

  • Breast cancer cell signaling and growth regulation.
  • Molecular and Cellular Biochemistry