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http://hdl.handle.net/2067/43162
Titolo: | Synthesis and Antiviral Activity of Novel 1,3,4-Thiadiazole Inhibitors of DDX3X | Autori: | botta, lorenzo annalaura brai Stefania Ronzini Valentina Riva Claudio Zamperini Matteo Borgini Claudia Immacolata Trivisani Anna Garbelli Carla Pennisi Adele Boccuto Francesco Saladini Maurizio Zazzi Giovanni Maga Maurizio Botta |
Rivista: | MOLECULES | Data pubblicazione: | 2019 | Abstract: | The human ATPase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against both infectious diseases and cancer. Herein, a new family of DDX3X inhibitors was designed, synthesized, and tested for its inhibitory action on the ATPase activity of the enzyme. The potential use of the most promising derivatives it has been investigated by evaluating their anti-HIV-1 e ects, revealing inhibitory activities in the low micromolar range. A preliminary ADME analysis demonstrated high metabolic stability and good aqueous solubility. The promising biological profile, together with the suitable in vitro pharmacokinetic properties, make these novel compounds a very good starting point for further development. |
URI: | http://hdl.handle.net/2067/43162 | ISSN: | 1420-3049 | DOI: | 10.3390/molecules24213988 | Diritti: | CC0 1.0 Universal |
È visualizzato nelle collezioni: | A1. Articolo in rivista |
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