Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents

	Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents
	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
	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
内容类型	期刊论文
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).