ml8b00605_si_001.pdf (1.67 MB)
Self-assembling Releasable Thiocolchicine–Diphenylbutenylaniline Conjugates
journal contribution
posted on 2019-01-04, 00:00 authored 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 PassarellaThe 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.