Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells

Simon E. Aspland, Carlo Ballatore, Rosario Castillo, Joel Desharnais, Trisha Eustaquio, Philip Goelet, Zijian Guo, Qing Li, David Nelson, Chengzao Sun, Angelo J. Castellino, Michael J. Newman

Research output: Contribution to journalArticlepeer-review

Abstract

In the present work, we explore the possibility of introducing selectivity to existing chemotherapeutics via the design of non-pro-drug, bi-functional molecules comprising a microtubule-binding agent and a substrate for a disease-associated kinase. The design, synthesis, and in vitro biological evaluation of paclitaxel-thymidine and vinblastine-thymidine bi-functional conjugates are reported here. This work provides the first account of 'kinase-mediated trapping' of cancer therapeutics.

Original languageEnglish (US)
Pages (from-to)5194-5198
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number19
DOIs
StatePublished - Oct 1 2006
Externally publishedYes

Keywords

  • Fluorescein
  • Kinase-mediated trapping
  • Paclitaxel
  • Thymidine
  • Thymidine kinase 1
  • Vinblastine

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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