Enhanced anticancer activity of multi-walled carbon nanotube-methotrexate conjugates using cleavable linkers.

Cristian Samorì (1) , Hanene Ali-Boucetta (2) , Raquel Sainz (1) , Chang Guo (2) , Francesca Maria Toma (3, 4) , Chiara Fabbro (3) , Tatiana da Ros (3) , Maurizio Prato (3) , Kostas Kostarelos (2) , Alberto Bianco (1)

1 ICT - Immunologie et chimie thérapeutiques
2 Nanomedicine Laboratory
3 Dipartimento di Scienze Farmaceutiche
4 SISSA / ISAS - Scuola Internazionale Superiore di Studi Avanzati / International School for Advanced Studies

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.

Domaines: Chimie thérapeutique

Cristian Samorì, Hanene Ali-Boucetta, Raquel Sainz, Chang Guo, Francesca Maria Toma, et al.. Enhanced anticancer activity of multi-walled carbon nanotube-methotrexate conjugates using cleavable linkers.. Chemical Communications, 2010, 46 (9), pp.1494-6. ⟨10.1039/b923560d⟩. ⟨hal-00468297⟩