Discovery of SIPI6473, a New, Potent, and Orally Bioavailable Multikinase Inhibitor for the Treatment of Non-small Cell Lung Cancer
نویسندگان
چکیده
A novel series of quinazoline derivatives were designed, synthesized, and evaluated as multikinase inhibitors. Most these compounds showed antiproliferation activities several human cancer cell lines exhibited inhibition efficacy against the estimated glomerular filtration rate (EGFR) in nanomolar level. Among those compounds, compound B5 (also named SIPI6473) displayed maximum effect, thus was chosen for further study. Our data revealed that inhibited activity kinases (such EGFR, VEGFR2, PDGFR?) contributed to development non-small lung (NSCLC). Besides, an vivo study also tumor growth without signs adverse effects A549 xenograft model. In conclusion, may represent a new promising drug treatment NSCLC.
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ژورنال
عنوان ژورنال: Pharmaceutical fronts
سال: 2021
ISSN: ['2628-5096', '2628-5088']
DOI: https://doi.org/10.1055/s-0041-1731081