title: Guanine-based amphiphiles: synthesis, ion transport properties and biological activity.
abstract: Novel amphiphilic guanine derivatives, here named Gua1 and Gua2, have been prepared through few, simple and efficient synthetic steps. In ion transport experiments through phospholipid bilayers, carried out to evaluate their ability to mediate H(+) transport, Gua2 showed high activity. When this compound was investigated for ion-selective transport activities, no major differences were observed in the behaviour with cations while, in the case of anions, selective activity was observed in the series I(-)>Br(-)>Cl(-)>F(-). The bioactivity of these guanine analogues has been evaluated on a panel of human tumour and non-tumour cell lines in preliminary in vitro cytotoxicity assays, showing a relevant antiproliferative profile for Gua2.
authors: Department of Chemical Sciences, University Federico II of Napoli, Via Cintia, 4, I-80126 Napoli, Italy.
authors: Domenica
authors: D
authors: Musumeci
authors: Department of Pharmacy, University Federico II of Napoli, Via D. Montesano, 49, I-80131 Napoli, Italy.
authors: Carlo
authors: C
authors: Irace
authors: Department of Pharmacy, University Federico II of Napoli, Via D. Montesano, 49, I-80131 Napoli, Italy.
authors: Rita
authors: R
authors: Santamaria
authors: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via L. Giorgieri, I-34127 Trieste, Italy.
authors: Domenico
authors: D
authors: Milano
authors: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via L. Giorgieri, I-34127 Trieste, Italy.
authors: Paolo
authors: P
authors: Tecilla
authors: Department of Chemical Sciences, University Federico II of Napoli, Via Cintia, 4, I-80126 Napoli, Italy. Electronic address: daniela.montesarchio@unina.it.
authors: Daniela
authors: D
authors: Montesarchio
mesh_terms: D002460:Cell Line; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006147:Guanine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D017136:Ion Transport
chemical_list: D006147:Guanine
keywords: Amphiphiles; Guanine derivatives; In vitro bioactivity tests; Synthetic ionophores