Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines. A series of ether, carbamate and ester derivatives was synthesized. All of them were studied and evaluated for their stability at different pH. The cytotoxic activity in vitro on NCI-H460 non-small cell lung carcinoma and A2780 ovarian tumor cell lines was also tested. A potential back-up of Adarotene has been selected to be evaluated in tumor models. --------------------------------------------------------------------------------
New retinoid derivatives as back-ups of Adarotene / G. Giannini, T. Brunetti, G. Battistuzzi, D. Alloatti, G. Quattrociocchi, M.G. Cima, L. Merlini, S. Dallavalle, R. Cincinelli, R. Nannei, L. Vesci, F. Bucci, R. Foderà, M.B. Guglielmi, C. Pisano, W. Cabri. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 20:7(2012), pp. 2405-2415.
New retinoid derivatives as back-ups of Adarotene
L. Merlini;S. Dallavalle;R. Cincinelli;R. Nannei;
2012
Abstract
Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines. A series of ether, carbamate and ester derivatives was synthesized. All of them were studied and evaluated for their stability at different pH. The cytotoxic activity in vitro on NCI-H460 non-small cell lung carcinoma and A2780 ovarian tumor cell lines was also tested. A potential back-up of Adarotene has been selected to be evaluated in tumor models. --------------------------------------------------------------------------------
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