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- W2476243668 abstract "After more than 20 years of research in the field of HDAC inhibitors, the oncological armamentarium has significantly enriched with new approved drugs. Currently, four drugs, Vorinostat (Zolinza; 2006), Romidepsin (Istodax; 2009) Belinostat (Beleodaq; 2014) and Panobinostat (Farydak; 2015) have been approved by the U.S. Food and Drug Administration (FDA) for the treatment of cutaneous T-cell lymphoma (CTCL), peripheral T-cell lymphoma (PTCL), and multiple myeloma, respectively. A fifth, Chidamide (Epidaza; 2015), has been recently approved by the China Food and Drug Administration for the treatment of PTCL. Beyond them, more than twenty are currently under pre-clinical and clinical investigation as single agent and in combination therapies against different cancers and in other several novel therapeutic indications. However, it is to emphasize a feature: among all these, no one, with the exception of the natural product Romidepsin, is a thiol derivative. After efforts lasted years, now we have selected ST7612AA1 - a new thiol-ω(γ-lactam amide) SAHA analogues, potential front-runner of a new generation of HDAC inhibitors, [1] highly competitive respect to other HDAC inhibitors drugs, orally administered with a negligible toxicity. ST7612AA1 displays low-nanomolar inhibitor activity on HDACs, being especially powerful on HDAC6 isoform, associated to a wide spectrum of antitumor activity, both in vitro and in vivo [2]; it can be industrially developed with a quick and easy synthetic process [3]. Moreover, it has also been investigated as an enhancer in antiretroviral therapy against HIV, aimed to eradicate the viral reservoirs [4]. All these results encouraged further enrichment experiments with ST7612AA1 as a drug candidate, which is currently in a phase of pre-clinical evaluation. The overall profile of ST7612AA1, including synthesis and a comprehensive pharmacological characterization, will be presented. [1] G. Giannini et al. J Med Chem. 2014, 57, 8358-8377 [2] L. Vesci et al. Oncotarget 2015, 6, 5735-48 [3] G. Battistuzzi, G. Giannini. Bioorg. Med. Chem .Lett. 2015, submitted [4] R. Badia Antiviral Research 2015, 123, 62-69 Citation Format: Giuseppe Giannini, Ferdinando Maria Milazzo, Gianfranco Battistuzzi, Loredana Vesci. ST7612AA1: focus on a drug candidate, front-runner of a new generation of HDAC inhibitors. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 4727." @default.
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- W2476243668 date "2016-07-15" @default.
- W2476243668 modified "2023-10-03" @default.
- W2476243668 title "Abstract 4727: ST7612AA1: focus on a drug candidate, front-runner of a new generation of HDAC inhibitors" @default.
- W2476243668 doi "https://doi.org/10.1158/1538-7445.am2016-4727" @default.
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