Gaia Fumagalli and Daniele Passarellaa
Department of Chemistry, University of Milan, Milano, Italy
An interesting research niche in cancer nanotechnology is represented by self-assembling drug conjugates that spontaneously form nanoparticles (NPs) in aqueous media. We recently reported the preparation of different types of NPs, starting from single drug-conjugates (1) and then combining two drug-conjugates and adding a fluorescent conjugate in order to trace the delivery. (2) In this scenario we moved our interest to self-assembly that possess an antiproliferative activity to make possible the obtainment of self-assembling dual drugs. We considered the use of the hydrophobic moiety of the 4-(1,2-diphenylbut-1-en-1-yl) aniline, a tamoxifen analog, which we recently demonstrated to have antiproliferative activity on different human tumor cell lines. (3) We prepared different conjugates containing aloin or podophyllotoxin and we demonstrated that they form NPs, confirming the propensity of 4-(1,2-diphenylbut-1-en-1-yl) aniline is able to induce self-assembly both when incorporated in amphiphilic and lipophilic conjugates. These NPs demonstrated a certain antiproliferative activity against different cell lines (4) .
S. Borrelli, M. S. Christodoulou, I. Ficarra, A. Silvani, G. Cappelletti, D. Cartelli, G. Damia, F. Ricci, M. Zucchetti, F. Dosio, D. Passarella, Eur.J. Med.Chem 2014, 15, 179-190.  S. Borrelli, D. Cartelli, F. Secundo, G. Fumagalli, M. S. Christodoulou, A. Borroni, F. Dosio, G. Cappelletti, D. Passarella ChemPlusChem 2015, 80, 47-49.  M.S. Christodoulou, M. Zarate, F. Ricci, G. Damia, S. Pieraccini, F. Dapiagg, M. Sironi, L. Lo Presti, A. N. García-Argaez, L. Dalla Via and D. Passarella Eur.J.Med.Chem. 2016, 118, 79-89.  G. Fumagalli, M.S. Christodoulou, B. Riva, I. Revuelta, C. Marucci, V. Collico, D. Prosperi, S. Riva, D. Perdicchia, I. Bassanini, A. García-Argáez, L. Dalla Via and D. Passarella Org. Biomol. Chem. 2017, 15, 1106-1109.
Keywords: Cancer, nanoparticles, self-assembling, drug-conjugates, tamoxifen.