2. Academic Validation
  3. Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells

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

  • Bioorg Med Chem Lett. 2006 Oct 1;16(19):5194-8. doi: 10.1016/j.bmcl.2006.07.003.
Simon E Aspland 1,  Carlo Ballatore,  Rosario Castillo,  Joel Desharnais,  Trisha Eustaquio,  Philip Goelet,  Zijian Guo,  Qing Li,  David Nelson,  Chengzao Sun,  Angelo J Castellino,  Michael J Newman
Affiliations

Affiliation

  • 1 Acidophil LLC, 2330 W. Joppa Road, Suite 330, Lutherville, MD 21093, USA. [email protected]
PMID: 16870428 DOI: 10.1016/j.bmcl.2006.07.003
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.

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