Discovery of novel polycyclic spiro-fused carbocyclicoxindole-based anticancer agents

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• 作者：Lidan Zhang^a ; ¹ ; Wen Ren^a ; ¹ ; Xiaoyan Wang^c ; Jiaying Zhang^d ; Jie Liu^a ; ^{liujie2011@scu.edu.cn} ; Lifeng Zhao^b ; ^{lifengzhao@scu.edu.cn} ; Xia Zhang^a ; ^{zhang-xia@scu.edu.cn}
• 关键词：Polycyclic spiro-fused carbocyclicoxindoles ; Antiproliferative activity ; p53 inducer ; MDM2
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：1071-1082
• 全文大小：2432 K
• 卷排序：126

文摘

Nineteen novel polycyclic spiro-fused carbocyclicoxindoles were investigated. Compound 10i displayed inhibitory activities against seven cancer cell lines. 10i arrested cell cycle in G1 phase and induced apoptosis. 10i enhanced the protein levels of cleaved caspase-3, p53, and MDM2. Docking studies showed 10i might block the MDM2-p53 interactions.