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- Title
Design, synthesis, and biological evaluation of urea‐based ROCK2 inhibitors.
- Authors
Wang, Linan; Qi, Junhui; Fan, Meixia; Yao, Lei
- Abstract
A series of urea‐based ROCK2 inhibitors were design and synthesized. The inhibitory activity on ROCK2 was screened by enzyme‐linked immunosorbent assay (ELISA). The study results showed that the urea derivatives exhibited certain ROCK2 inhibitory activity. The most potent compound 10p showed ROCK2 inhibitory activity with the IC50 value of 0.03 μM. A preliminary structure‐activity relationship was then summarized. The molecular docking studies showed that further optimization needs to conduct to obtain more potent ROCK inhibitors.
- Subjects
UREA derivatives; ENZYME-linked immunosorbent assay; MOLECULAR docking; UREA; STRUCTURE-activity relationships
- Publication
Chemical Biology & Drug Design, 2021, Vol 98, Issue 6, p969
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13961