Synthesis and Antiviral Activity of Novel 1,3,4-Thiadiazole Inhibitors of DDX3X
Author(s)
Date Issued
2019
Type
article
Volume
24
Issue
21
Start Page
1
End Page
18
Journal
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.
Subjects