期刊
MOLECULES
卷 24, 期 21, 页码 -出版社
MDPI
DOI: 10.3390/molecules24213988
关键词
DDX3X; HIV-1; host proteins; antivirals
资金
- First Health Pharmaceutical B.V
- CNR Project Identification of novel molecules with therapeutic potential against Zika virus and other emerging viruses
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 effects, 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.
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