AI Article Synopsis
- A total of 29 new compounds featuring N-(2-aryl-1, 3-thiazolidin-4-one)-N-aryl ureas were created and tested for biological activity.
- The study clarified the structure-activity relationships (SARs) and how these compounds bind to their targets.
- Among the compounds, 29b showed strong effectiveness against several multi-tyrosine kinases and was confirmed to inhibit growth and kill A549 cancer cells using live-cell imaging technology.
Article Abstract
A total of 29 novel compounds bearing N-(2-aryl-1, 3-thiazolidin-4-one)-N-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was identified possessing high potency against multi-tyrosine kinases including Ron, c-Met, c-Kit, KDR, Src and IGF-1R, etc. In vitro antiproliferation and cytotoxicity of compound 29b against A549 cancer cell line were confirmed by IncuCyte live-cell imaging.
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| http://dx.doi.org/10.1016/j.ejmech.2018.01.061 | DOI Listing |
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