The Design, Synthesis, and Biological Evaluation of New Paclitaxel Analogs With the Ability to Evade Efflux by P-Glycoprotein

Abstract

Regioisomeric functional group and one-carbon homologs of the semi-synthetic paclitaxel compound TX-67 (C10 hemi- succinate) have been prepared to investigate its lack of interaction with P-glycoprotein (Pgp). In accord with Seelig's model and our previous reports all carboxylic acid analogs had no apparent interactions with Pgp. Furthermore it is demonstrated that hydrogen-bonding properties were significant with respect to Pgp interactions. This anionic introduction strategy may allow for delivery of paclitaxel into the CNS as well as establishing an alternative strategy for delivery of other non-CNS permeable drugs.

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Document Details

Document Type
Technical Report
Publication Date
May 01, 2005
Accession Number
ADA472618

Entities

People

  • Brandon J. Turunen

Organizations

  • University of Kansas

Tags

DTIC Thesaurus Topics

  • Alzheimer Disease
  • Blood
  • Carboxylic Acids
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Neurodegeneration
  • Neurodegenerative Diseases
  • Organic Chemistry
  • Proteins

Fields of Study

  • Chemistry

Readers

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