Synthesis of Cryptophycin Affinity Labels and Tubulin Labeling

Abstract

Cryptophycins are a potent, tumor-selective class of tubulin-binding antimitotic anticancer agents with excellent activity against MDR cancers. For the development of these promising compounds into useful chemotherapeutic agents, detailed information about the binding domain of the cryptophycins is essential. We plan to map the cryptophycin binding site through photoaffinity labeling studies. Toward this goal we have prepared ClO azido analogues of cryptophycin-24 and have evaluated them in a tubulin assembly assay. We have found them to be potential candidates for photoaffinity labeling studies.

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Document Details

Document Type
Technical Report
Publication Date
May 01, 2004
Accession Number
ADA432471

Entities

People

  • Agunda I. Georg
  • Kyounglang Yang

Organizations

  • University of Kansas

Tags

Communities of Interest

  • Biomedical

DTIC Thesaurus Topics

  • Abstracts
  • Amides
  • Amino Acids
  • Analogs
  • Antineoplastic Agents
  • Assembly
  • Biochemistry
  • Cell Line
  • Chemical Synthesis
  • Chemistry
  • Chemotherapeutic Agents
  • Column Chromatography
  • Cyanobacteria
  • Materials
  • Neoplasms
  • Organic Chemistry
  • Tumor Cell Line

Fields of Study

  • Chemistry
  • Computer science

Readers

  • Molecular and Cellular Biochemistry
  • Oncology (Cancer Research).