116465-58-8Relevant articles and documents
DDX3X Helicase Inhibitors as a New Strategy to Fight the West Nile Virus Infection
Brai, Annalaura,Martelli, Francesco,Riva, Valentina,Garbelli, Anna,Fazi, Roberta,Zamperini, Claudio,Pollutri, Alessandro,Falsitta, Lucia,Ronzini, Stefania,Maccari, Laura,Maga, Giovanni,Giannecchini, Simone,Botta, Maurizio
, p. 2333 - 2347 (2019)
Increased frequency of arbovirus outbreaks in the last 10 years represents an important emergence for global health. Climate warming, extensive urbanization of tropical regions, and human migration flows facilitate the expansion of anthropophilic mosquitos and the emerging or re-emerging of new viral infections. Only recently the human adenosinetriphosphatase/RNA helicase X-linked DEAD-box polypeptide 3 (DDX3X) emerged as a novel therapeutic target in the fight against infectious diseases. Herein, starting from our previous studies, a new family of DDX3X inhibitors was designed, synthesized, validated on the target enzyme, and evaluated against the West Nile virus (WNV) infection. Time of addition experiments after virus infection indicated that the compounds exerted their antiviral activities after the entry process, likely at the protein translation step of WNV replication. Finally, the most interesting compounds were then analyzed for their in vitro pharmacokinetic parameters, revealing favorable absorption, distribution, metabolism, and excretion values. The good safety profile together with a good activity against WNV for which no treatments are currently available, make this new class of molecules a good starting point for further in vivo studies.
USE OF DDX3 INHIBITORS AS ANTIPROLIFERATIVE AGENTS
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Page/Page column 69; 70; 72, (2017/10/30)
The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)
HUMAN HELICASE DDX3 INHIBITORS AS THERAPEUTIC AGENTS
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Page/Page column 79; 80, (2016/09/22)
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.