Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents
文献类型：期刊论文
| 作者 | Peng, Yuefeng; Sun, Haiying; Lu, Jianfeng; Liu, Liu; Cai, Qian; Shen, Rong; Yang, Chao-Yie; Yi, Han; Wang, Shaomeng |
| 刊名 | Journal of medicinal chemistry
 |
| 出版日期 | 2012 |
| 英文摘要 | Nonpeptidic, bivalent Smac mimetics designed based upon monovalent Smac mimetics with a diazabicyclic core structure bind to XIAP, cIAP1, and cIAP2with low to subnanomolar affinities and are highly effective in antagonizing XIAP in cell-free functional assays. They efficiently induce the degradation of cIAP1and cIAP2 in cancer cells at concentrations as low as 1 nM, activate caspase-3 and -8, and cleave PARP at 3-10 nM. The most potent compounds in the series have IC50 of 3-5 nM in inhibition of cell growth in both MDA-MB-231and SK-OV-3 cell lines and are promising lead compounds for the development of anew class of cancer therapy. |
| 收录类别 | SCI |
| 原文出处 | http://pubs.acs.org/doi/pdf/10.1021/jm201072x |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/4268]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 作者单位 | Journal of medicinal chemistry |
| 推荐引用方式 GB/T 7714 | Peng, Yuefeng,Sun, Haiying,Lu, Jianfeng,et al. Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents[J]. Journal of medicinal chemistry,2012. |
| APA | Peng, Yuefeng.,Sun, Haiying.,Lu, Jianfeng.,Liu, Liu.,Cai, Qian.,...&Wang, Shaomeng.(2012).Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.Journal of medicinal chemistry. |
| MLA | Peng, Yuefeng,et al."Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents".Journal of medicinal chemistry (2012). |
入库方式： OAI收割
来源：深圳先进技术研究院
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