Design and Synthesis of New Breast Cancer Chemotherapeutic Agents

Abstract

This proposal is directed towards the development of new chemotherapeutic agents based on the mechanism of action of Taxol. The recent discovery of two other natural products, epothilone and discodermolide, that operate by the same unique mechanism of action as Taxol, i.e., microtubule stabilization, provides a unique opportunity for a collaborative approach using synthetic and computational studies for the elucidation of the pharmacophore common to these structurally dissimilar substances. Such an advance could lead to the development of a novel family of breast cancer chemotherapeutics. We describe herein the synthesis and biological evaluation of novel analogs of the potent antitumor agent epothilone. Our results indicate that these partial structures do not have sufficient similarity to the natural product for biological activity.

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Document Details

Document Type
Technical Report
Publication Date
Aug 01, 1999
Accession Number
ADB259031

Entities

People

  • Jeffrey D. Winkler

Organizations

  • University of Pennsylvania

Tags

Communities of Interest

  • Biomedical

DTIC Thesaurus Topics

  • Alkanes
  • Alkenes
  • Antineoplastic Agents
  • Biological Products
  • Breast Cancer
  • Chemical Synthesis
  • Chemistry
  • Chemotherapeutic Agents
  • Chlorides
  • Neoplasms
  • Organic Chemistry

Fields of Study

  • Chemistry

Readers

  • Molecular and Cellular Biochemistry
  • Oncology (Cancer Research).
  • Systems Analysis and Design