DNA Topoisomerase I-Targeted Therapy for Breast Cancer

Abstract

Camptothecin analogues have been developed that show enhanced pre-clinical activity against breast cancer cells. These analogues have been synthesized with two fundamental modifications that aid in their effectiveness against breast cancer: (1) they have a glycinate ester of the 20(S)-OH group, which aids in both solubility and stabilization of the drug's lactone ring; and (2) they possess a 9-chloro substitution, which allows them to covalently link to DNA. We have studied the activity of these compounds against breast cancer cells in a series of in vitro tests: growth inhibitory activity, clonogenic survival assays, and inhibition of topoisomerase I catalytic activity.

Open PDF

Document Details

Document Type
Technical Report
Publication Date
Jun 01, 1997
Accession Number
ADB225820

Entities

People

  • Daniel D. Von Hoff
  • Shi-fon Chen

Tags

DTIC Thesaurus Topics

  • Antineoplastic Agents
  • Biomedical Research
  • Breast Cancer
  • Carcinoma
  • Cell Line
  • Cells
  • Chemistry
  • Chemotherapy
  • Clinical Trials
  • Culture Techniques
  • Enzyme Inhibitors
  • Indicator Dyes
  • Lung Cancer
  • Neoplasms
  • Resistance
  • Tumor Cell Line
  • United States

Fields of Study

  • Chemistry

Readers

  • Molecular Biology and Genetics
  • Oncology (Cancer Research).
  • Organic Chemistry