Synthesis of Cryptophycin Affinity Labels and Tubulin Labeling

Abstract

Cryptophycins are a potent tumor-selective class of tubulin-binding antimitotic anti-cancer agents with excellent activity against MDR cancers. In order to develop these promising compounds into useful chemotherapeutic agents it is necessary to obtain detailed information about the binding domain of the cryptophycins on tubulin. We plan to map the cryptophycin binding site through photoaffinity labeling studies. Toward this goal, we have synthesized and studied the activity of C16 side chain azido analogues and synthesized C6 dimethyl and C10 azido analogues of cryptophycin-24, by means of inventing an improved synthetic route to achieve the synthesis of diverse analogues in a more efficient way.

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Document Details

Document Type
Technical Report
Publication Date
May 01, 2006
Accession Number
ADA474734

Entities

People

  • Gunda I. Georg
  • Kyounglang Yang

Organizations

  • University of Kansas

Tags

DTIC Thesaurus Topics

  • Analogs
  • Antineoplastic Agents
  • Assembly
  • Biomedical Research
  • Cell Line
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Chemotherapeutic Agents
  • Couplings
  • Culture Techniques
  • Cyanobacteria
  • Data Analysis
  • Ketones
  • Molecules
  • Neoplasms
  • Proteins

Fields of Study

  • Chemistry
  • Computer science

Readers

  • Molecular and Cellular Biochemistry