作者: Carlos J.A. Ribeiro , Joana D. Amaral , Cecília M.P. Rodrigues , Rui Moreira , Maria M.M. Santos
DOI: 10.1016/J.BMC.2013.10.048
关键词: Biochemistry 、 Cell growth 、 Bimolecular fluorescence complementation 、 Chemistry 、 Protein–protein interaction 、 Mdm2 、 Cancer 、 Programmed cell death 、 Apoptosis
摘要: Restoring p53 levels through disruption of p53-MDM2 interaction has been proved to be a valuable approach in fighting cancer. We herein report the synthesis and evaluation eighteen spiroisoxazoline oxindoles derivatives as inhibitors. Seven compounds showed an antiproliferative profile superior inhibitor nutlin-3, induced cell death by apoptosis. Moreover, proof-of-concept was demonstrated inhibition between MDM2 live-cell bimolecular fluorescence complementation assay.