Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 20, Issue 52, Pages 17541-17551Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201404502
Keywords
antitumor agents; hyperthermia; maytansinoids; mutasynthesis; nanoparticles
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Funding
- Deutsche Forschungsgemeinschaft (Cluster of Excellence REBIRTH) [EXC 62]
- Ministry of Science and Culture of Lower Saxony
- Fonds der Chemischen Industrie
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A combination of mutasynthesis, precursor-directed biosynthesis and semisynthesis provides access to new ansamitocin derivatives including new nanostructured particle-drug conjugates. These conjugates are based on the toxin ansamitocin and superparamagnetic iron oxide-silica core shell particles. New ansamitocin derivatives that are functionalized either with alkynyl- or azido groups in the ester side chain at C-3 are attached to nanostructured iron oxide core-silica shell particles. Upon exposure to an oscillating electromagnetic field these conjugates heat up and the ansamitocin derivatives are released by a retro-Diels-Alder reaction. For example, one ansamitocin derivative exerts strong antiproliferative activity against various cancer cell lines in the lower nanomolar range while the corresponding nanostructured particle-drug conjugate is not toxic. Therefore, these new conjugates can serve as dormant toxins that can be employed simultaneously in hyperthermia and chemotherapy when external inductive heating is applied.
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