Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents

• Twenty seven novel diaryl ureas were designed and synthesized.
• Their antitumor activity against five cancer cell lines was evaluated.
• Compound 23 demonstrated broad-spectrum antitumor activity in vitro.
• Compound 23 was subjected to docking analysis on B-Raf.
• Compound 23 was screened for Raf kinase inhibition.

A novel series of diaryl ureas containing different linker groups were designed and synthesized. Their in vitro antitumor activity against MX-1, A375, HepG2, Ketr3 and HT-29 was evaluated using the standard MTT assay. Compounds having a rigid linker group such as vinyl, ethynyl and phenyl showed significant inhibitory activity against a variety of cancer cell lines. Specifically, compound 23 with a phenyl linker group demonstrated broad-spectrum antitumor activity with IC50 values of 5.17–6.46 μM against five tested tumor cell lines. Compound 23 is more potent than reference drug sorafenib (8.27–15.2 μM), representing a promising lead for further optimization.

A series of diaryl urea derivatives containing different linker groups were designed and synthesized. Compound 23 demonstrated broad-spectrum antitumor activity in vitro.Figure optionsDownload as PowerPoint slide