Self-assembled nanoparticles: anticancer natural products as building blocks

Italian
Abstract: 
Our continuous interest in the field of chemical approaches to target cancer cells moved us to study the preparation of a novel classes of conjugate compounds using anticancer drugs as building blocks. In previous efforts we used squalene tail as self-assembling inducer1 and a disulphide containing linker to secure the release of the drugs after cell internalization.2 Subsequently we demonstrated the possibility to generate hetero and fluorescent nanoparticles by mixing a paclitaxel-squalene conjugate and fluorescein-squalene conjugate.3 In the light of facing the high demanding issue of resistance4 we studied the formation of cyclopamine-paclitaxel containing nanoparticles and we detected the internalization by confocal microscopy and super-resolution.5 More recently we reported doxorubicin-cyclopamine hetero-nanoparticles that are able to reduce tumour growth and to decrease the toxicity of chemotherapy in mice.6 Our efforts are actually focused on: a) new self-assembling inducers,7 b) new combination of drugs to overcome drug resistance,9 c) new hetero-nanoparticles and d) new drug-conjugates deriving by modification of active natural products. 
 
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4. P.A. Sotiropoulou, C. Herold-Mende, D. Passarella et al.  Drug Discovery Today 2014, 19, 1547 
5. G. Fumagalli, D. Passarella et al.  ChemPlusChem 2015, 9, 1380
6. G. Fumagalli, D. Passarella et al.  ACS Med. Chem. Lett. 2017, 8, 953
7. G. Fumagalli, D. Passarella et al.  Org. Biomol. Chem., 2017, 15, 1106
8. G. Fumagalli, D. Passarella et al.  ACS Med. Chem. Lett. 2018, 9, 468

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