Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold

A series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and HepG2 cell lines using Sorafenib as the positive control. Compounds 6i showed a good to moderate inhibition on VEGFR-2 and PI3Kα which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.

Graphical abstractA series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were synthesized, which demonstrated potency against both MDA-MB-231 and HepG2 cell lines. Compound 6i is identified as a potentially dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.Figure optionsDownload full-size imageDownload as PowerPoint slide