title: New retinoid derivatives as back-ups of Adarotene.
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.
authors.affiliation: Sigma-Tau Industrie Farmaceutiche Riunite Spa, via Pontina Km 30.400, 00040 Pomezia, Italy. giuseppe.giannini@sigma-tau.it
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Giannini
authors.forename: Tiziana
authors.initials: T
authors.lastname: Brunetti
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Battistuzzi
authors.forename: Domenico
authors.initials: D
authors.lastname: Alloatti
authors.forename: Gianandrea
authors.initials: G
authors.lastname: Quattrociocchi
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Cima
authors.forename: Lucio
authors.initials: L
authors.lastname: Merlini
authors.forename: Sabrina
authors.initials: S
authors.lastname: Dallavalle
authors.forename: Raffaella
authors.initials: R
authors.lastname: Cincinelli
authors.forename: Raffaella
authors.initials: R
authors.lastname: Nannei
authors.forename: Loredana
authors.initials: L
authors.lastname: Vesci
authors.forename: Federica
authors.initials: F
authors.lastname: Bucci
authors.forename: Rosanna
authors.initials: R
authors.lastname: Foderà
authors.forename: Mario Berardino
authors.initials: MB
authors.lastname: Guglielmi
authors.forename: Claudio
authors.initials: C
authors.lastname: Pisano
authors.forename: Walter
authors.initials: W
authors.lastname: Cabri
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D002289:Carcinoma, Non-Small-Cell Lung / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004950:Esterases / Q000378:metabolism; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D008819:Mice, Nude; D012176:Retinoids / Q000737:chemistry* / Q000494:pharmacology / Q000633:toxicity; D014183:Transplantation, Heterologous
chemical_list: D000970:Antineoplastic Agents; D012176:Retinoids; D004950:Esterases; C573390:adarotene