C-7 Progesterone Analogues and MDR1 in Breast Cancer

Abstract

We have generated novel analogs of progesterone (PgA) as potent inhibitors of the MDR1 multidrug resistant phenotype in breast cancer. The objectives of this Research Project include the optimization of the PgA's MDR1-reversing activity through the generation of additional compounds, using an analog design approach, the definition of these compounds' in vivo efficacy, and of their mechanism of action. In the course of the fourth year of the Project, we have: 1) tested the in vivo MDR-reversing activity of PgA4, the most potent among our initial progesterone analogs; 2) designed and synthesized additional progesterone analogs and evaluated their structure-activity relationships; 3) related the in vitro activity of some of the analogs to their in vitro toxicity.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2001
Accession Number
ADA398655

Entities

People

  • Robert R. Clarke

Organizations

  • Georgetown University

Tags

DTIC Thesaurus Topics

  • Antineoplastic Agents
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Health Services
  • Lymphocytes
  • Medical Personnel
  • Organic Chemistry

Fields of Study

  • Chemistry

Readers

  • Breast cancer cell signaling and growth regulation.
  • Computer Engineering
  • Neurotoxicology