A Novel Approach to Prostate Cancer Chemotherapy: Design of Prodrugs for Tissue-Specific Activation

Abstract

During the second year of funding, we determined the stability of two 5-FU Linker-Drug conjugates originally designed and found them to be unstable and not suitable for incorporation into prodrugs. We modified the structure and synthesized two new linkers. The new Linker-Drug conjugates of 5-FU were found to be stable under physiological conditions in the masked form and could undergo once unmasked the cyclization activation process as originally proposed to release the drug 5-FU. We also accomplished the synthesis of a Peptide-Linker-Drug conjugate albeit with an unstable linker. But, the chemistry developed will be useful for the construction of more promising Peptide-Linker-Drug conjugates.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2001
Accession Number
ADB282347

Entities

People

  • Longgin Hu

Organizations

  • Rutgers University–New Brunswick

Tags

DTIC Thesaurus Topics

  • Alkanes
  • Amines
  • Cancer
  • Chemical Synthesis
  • Chemistry
  • Chemotherapy
  • Chlorides
  • Ethers
  • Health Services
  • Hydrogen
  • Hydroxides
  • Neoplasms
  • Organic Chemistry
  • Prostate Cancer

Fields of Study

  • Chemistry

Readers

  • Molecular and Cellular Biochemistry
  • Research Science/Academic Research