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Enhanced Anticancer Activity of Multi-walled Carbon Nanotube-methotrexate Conjugates Using Cleavable Linkers

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Samorì C, Ali-Boucetta H, Sainz R, Guo C, Toma FM, Fabbro C, da Ros T, Prato M, Kostarelos K, Bianco A.

CNRS, Institut de Biologie Moléculaire et Cellulaire, Laboratoire d’Immunologie et Chimie Thérapeutiques, 67000 Strasbourg, France.

Methotrexate was tethered to multi-walled carbon nanotubes through different cleavable linkers exploiting the ammonium functionalities introduced by 1,3-dipolar cycloaddition reaction of azomethine ylides to the nanotubes. The new nanobio-hybrid conjugates were internalized into human breast cancer cells and it was shown that the cytotoxic activity was strongly dependent on the presence and type of linker.
Chem Commun (Camb). 2010 Mar 7;46(9):1494-6. Epub 2009 Dec 23.

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