Bioorganic and Medicinal Chemistry Letters p. 5194 - 5198 (2006)
Update date:2022-08-04
Topics:
Aspland, Simon E.
Ballatore, Carlo
Castillo, Rosario
Desharnais, Joel
Eustaquio, Trisha
Goelet, Philip
Guo, Zijian
Li, Qing
Nelson, David
Sun, Chengzao
Castellino, Angelo J.
Newman, Michael J.
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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