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Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold
Authors:Lin Li  Cun-Long Zhang  Hong-Rui Song  Chun-Yan Tan  Huai-Wei Ding  Yu-Yang Jiang
Affiliation:a Department of Chemistry, Tsinghua University, Beijing 100084, China; b School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110000, China; c The Graduate School at Shenzhen, Tsinghua University, Shenzhen 518000, China
Abstract: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.
Keywords:2-Aminothiazole  VEGFR  PI3K  Anticancer  
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