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Potent anticancer prodrugs able to self-assemble after conjugation with squalene moiety. Role of the releasing spacer (Next-SQ-CancerDrugs)

Docente
Dott. Barbara STELLA
Coordinatore/trice
Prof. Franco DOSIO

Aree / Gruppi di ricerca

Partecipanti al progetto

Descrizione del progetto

Members of other units:
Daniele Passarella (Organic Chem. Dept.UniMi) 
Stella Borrelli (Organic Chem. Dept. UniMi)
Giovanna Damia (Mario Negri Inst.)
Graziella Cappelletti (Bioscience Dept, UniMi)

Sponsors:
Local funds (ex_60%) University of Turin, Italy   
University of Milan, Italy 

Description
This project is based on the synthesis of novel classes of squalene bioconjugates: these compounds contain a squalene tail, that makes them able to self-assemble in water, and a drug unit connected via a easily releasable linker  inside cells. The approach allows the release of active drug through reducible linkages as well as spacer/linker activated through enzymatic hydrolysis. Several potent anticancer drugs are screened  (taxanes, podophillotoxins, epothilones, colchicine, camptotechin derivatives etc).  All the squalenoyl prodrugs can be able to self-assemble and the obtained nanoparticles are fully characterized from a technological point of view. All compounds are evaluated through cell tests and the best candidates are going to be submitted to preclinical evaluation.

References:
- Dosio F et al , 2010. Bioconj. Chem  21, 1349-1361
- Couvreur P. et al 2010 US2010305030
- Passarella D. et al 2010. Eur.J.Med.Chem. 45, 219-226

Keywords:
Anticancer agents, Squalenoyl derivatives, Nanoparticles, Taxanes, Epothilones, Camptotechin

Ultimo aggiornamento: 30/03/2015 15:54
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