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Metastatic cancer is considered a fatal progression of cancer worldwide. It has been shown that a key player in this scenario is the CXC chemokine receptor 2 (CXCR2). To identify novel CXCR2 antagonists, a pharmacophore model was built with the H ip H op  program by screening a database containing compounds which were designed based on the known structure–activity relationship (SAR) of the diarylurea series CXCR2 antagonists. Compound  1a  bearing the novel skeleton was selected from database screening and subjected to the  in vitro  biological test which showed a moderate CXCR2 antagonist potential. With further modification and exploration of SAR, compound  1e  demonstrated improved CXCR2 antagonist activity with an IC 50  value of 14.8 µM. Furthermore, wound healing assay using the NCI-H1299 cell line indicated that  1e  showed an excellent anti-cancer metastatic effect (72% inhibition in cell migration at 50 µg ml −1 ).

Ligand-based pharmacophore model for the discovery of novel CXCR2 antagonists as anti-cancer metastatic agents