1232884-88-6Relevant articles and documents
New retinoid derivatives as back-ups of Adarotene
Giannini, Giuseppe,Brunetti, Tiziana,Battistuzzi, Gianfranco,Alloatti, Domenico,Quattrociocchi, Gianandrea,Cima, Maria Grazia,Merlini, Lucio,Dallavalle, Sabrina,Cincinelli, Raffaella,Nannei, Raffaella,Vesci, Loredana,Bucci, Federica,Foderà, Rosanna,Guglielmi, Mario Berardino,Pisano, Claudio,Cabri, Walter
, p. 2405 - 2415 (2012/05/07)
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.
