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 language | English (US) |
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Pages (from-to) | 5194-5198 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 19 |
DOIs | |
State | Published - Oct 1 2006 |
Externally published | Yes |
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