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Tebrophen — An Old Polyphenol Drug with Anticancer Potential †
Laboratory for Molecular and Cellular Biology, Division of Molecular Biology, Ruđer Bošković Institute, Bijenička cesta 54, HR-10000 Zagreb, Croatia
GlaxoSmithKline Research Centre Zagreb Ltd., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
Laboratory for Epigenomics, Division of Molecular Medicine, Ruđer Bošković Institute, Bijenička cesta 54, HR-10000 Zagreb, Croatia
Galapagos istraživački centar d.o.o., Prilaz baruna Filipovića 29, HR-10000 Zagreb, Croatia
University of Zagreb, School of Medicine, Center for Translational and Clinical Research, Šalata 2, HR-10000 Zagreb, Croatia
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* Author to whom correspondence should be addressed.
Received: 26 March 2012; in revised form: 8 June 2012 / Accepted: 14 June 2012 / Published: 28 June 2012
Abstract: In vitro high-throughput screening was carried out in order to detect new activities for old drugs and to select compounds for the drug development process comprising new indications. Tebrophen, a known antiviral drug, was found to inhibit activities on inflammation and cancer related targets. In primary screening this semisynthetic halogenated polyphenol was identified to inhibit the activities of kinases ZAP-70 and Lck (IC50 0.34 µM and 16 µM, respectively), as well as hydrolase DPPIV (at 80 µM 41% inhibition). Next, it showed no cytotoxic effects on standard cell lines within 24 h. However, tebrophen slowed propagation of breast cancer (MDA-MB-231), osteosarcoma (U2OS) and cervical carcinoma (HeLa), through at least 35 population doublings in a dose-dependent manner. It completely stopped the division of the prostate cancer (PC3) cell line at 50 µM concentration and the cells entered massive cell death in less than 20 days. On the other hand, tebrophen did not influence the growth of normal fibroblasts. According to the measured oxidative burst and estimated in silico parameters its direct antioxidative ability is limited. The obtained results indicate that tebrophen can be considered a promising lead molecule for generating more soluble derivatives with specific anticancer efficacy.
Keywords: tebrophen; anticancer; high-throughput screening; molecular modelling; population doublings
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Rubelj, I.; Stepanić, V.; Jelić, D.; Vidaček, N.Š.; Kalajžić, A.Ć.; Ivanković, M.; Nujić, K.; Matijašić, M.; Verbanac, D. Tebrophen — An Old Polyphenol Drug with Anticancer Potential †. Molecules 2012, 17, 7864-7886.
Rubelj I, Stepanić V, Jelić D, Vidaček NŠ, Kalajžić AĆ, Ivanković M, Nujić K, Matijašić M, Verbanac D. Tebrophen — An Old Polyphenol Drug with Anticancer Potential †. Molecules. 2012; 17(7):7864-7886.
Rubelj, Ivica; Stepanić, Višnja; Jelić, Dubravko; Vidaček, Nikolina Škrobot; Kalajžić, Andrea Ćukušić; Ivanković, Milena; Nujić, Krunoslav; Matijašić, Mario; Verbanac, Donatella. 2012. "Tebrophen — An Old Polyphenol Drug with Anticancer Potential †." Molecules 17, no. 7: 7864-7886.