2. Academic Validation
  3. Self-assembling Releasable Thiocolchicine-Diphenylbutenylaniline Conjugates

Self-assembling Releasable Thiocolchicine-Diphenylbutenylaniline Conjugates

  • ACS Med Chem Lett. 2019 Jan 4;10(4):611-614. doi: 10.1021/acsmedchemlett.8b00605.
Gaia Fumagalli 1,  Laura Polito 2,  Eleonora Colombo 1,  Francesca Foschi 1,  Michael S Christodoulou 1,  Francesco Galeotti 3,  Dario Perdicchia 1,  Ivan Bassanini 4,  Sergio Riva 4,  Pierfausto Seneci 1,  Aída García-Argáez 5 6,  Lisa Dalla Via 5,  Daniele Passarella 1
Affiliations

Affiliations

  • 1 Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.
  • 2 CNR-ISTM, Via G. Fantoli 16/15, 20138 Milano, Italy.
  • 3 CNR-ISMAC, Via A. Corti 12, 20133 Milano, Italy.
  • 4 Istituto di Chimica del Riconoscimento Molecolare-C.N.R.-ICRM, Via Mario Bianco 9, 20131 Milano, Italy.
  • 5 Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, Via F. Marzolo 5, 35131 Padova, Italy.
  • 6 Fondazione per la Biologia e la Medicina della Rigenerazione T.E.S.-Tissue Engineering and Signalling Onlus, Via F. Marzolo 13, 35131 Padova, Italy.
PMID: 30996805 DOI: 10.1021/acsmedchemlett.8b00605
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.

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