Natural Products as Building Blocks for Self-assembled Nanoparticles

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 had the way to detect the internalization by confocal microscopy and super-resolution.5 Our efforts are actually focused on: a) new combination of drugs to overcome drug resistance, b) new self-assembling inducers,6 c) new hetero-nanoparticles7 and d) new drug-conjugates deriving by modification of active natural products. References: 1. G. Fumagalli,D. Passarella et al. Drug Discovery Today 2016, 21, 1321 2. S. Borrelli, A. D. Passarella et al. Eur.J.Med.Chem 2014, 85, 179 3. G. Fumagalli, D. Passarella et al. ChemPlusChem 2015, 80, 47 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, M.S. Christodoulou, D. Passarella et al. Org. Biomol. Chem. 2017 DOI: 10.1039/c6ob02591a 7. G. Fumagalli, M.S. Christodoulou, D. Passarella et al. Paper submitted