Psoriasis, which severely affects the sufferer's life quality, is a chronic skin disease still lacking satisfactory medication. Recently, signal transducer and activator of transcription 3 (STAT3) was revealed playing an important role in the progression of psoriasis. In this paper, a total of 59 quinone derivatives with various scaffolds were designed, synthesized, and evaluated for antipsoriatic potential as STAT3 inhibitors. Among them, was identified as the most potent antipsoriatic agent and could bind to STAT3; reduce both total and phosphorylated STAT3 levels, inhibit the nuclear translocation of STAT3; and, therefore, inhibit the transcription and expression of the propsoriatic factor IL-17A. experiments on mice showed that the topical application of was effective in alleviating IMQ-induced psoriasis without noticeable side effects. In all, this research rendered as a promising drug candidate for psoriasis.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1021/acs.jmedchem.4c01055 | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!