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Self-assembling Releasable Thiocolchicine–Diphenylbutenylaniline Conjugates

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journal contribution
posted on 04.01.2019, 00:00 by Gaia Fumagalli, Laura Polito, Eleonora Colombo, Francesca Foschi, Michael S. Christodoulou, Francesco Galeotti, Dario Perdicchia, Ivan Bassanini, Sergio Riva, Pierfausto Seneci, Aída García-Argáez, Lisa Dalla Via, Daniele Passarella
The design and the synthesis of new self-assembling conjugates is reported. The target compounds are characterized by the presence of a self-immolative linker that secures a controlled release induced by lipase cleavage. 4-(1,2-Diphenylbut-1-en-1-yl)­aniline is used as a self-assembling inducer and amino-thiocolchicine as prototype of drug. The release of thiocolchicine derivative has been demonstrated in vitro in the presence of porcine pancreatic lipase and Celite-supported lipase. The formation of nanoparticles is confirmed by dynamic light scattering, atomic force microscopy, and fluorescence microscopy. The antiproliferative activity has been proved on two human cancer cell lines.