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Self-assembling Releasable Thiocolchicine-Diphenylbutenylaniline Conjugates

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, etc.

ACS Med Chem Lett. 2019 Jan 4;10(4):611-614.

PMID: 30996805

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP2730714 Thiocolchicine Thiocolchicine 2730-71-4 Price
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