Integrated bioinformatics, computational and experimental methods to discover novel Raf/extracellular-signal regulated kinase (ERK) dual inhibitors against breast cancer cells

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• 作者：Yin Chen^a ; ¹ ; Yaxin Zheng^a ; ¹ ; Qinglin Jiang^a ; ^b ; ¹ ; Feifei Qin^a ; Yonghui Zhang^c ; Leilei Fu^a ; ^{leilei_fu@163.com} ; Gu He^a ; ^{hegu@scu.edu.cn}
• 关键词：Breast cancer ; Raf ; ERK ; Bioinformatics ; Kinase inhibitor
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：997-1011
• 全文大小：2767 K
• 卷排序：127

文摘

30 compounds were designed as novel Raf1/ERK dual inhibitors and tested for their antiproliferative activity. Compound 9d showed significant IC50 at sub-micromolar level both in kinase inhibitory and cell proliferation assays. Compound 9d induces mitochondria apoptosis. These can be considered as interesting lead molecules against breast cancer.