Antitumor Activity of a 5-Hydroxy-1H-Pyrrol-2-(5H)-One-Based Synthetic Small Molecule In Vitro and In Vivo

	Antitumor Activity of a 5-Hydroxy-1H-Pyrrol-2-(5H)-One-Based Synthetic Small Molecule In Vitro and In Vivo
	Geng, Yunyun 1,2; Wang, Xiaojian 1,2; Yang, Luo 3; Sun, Haili 1,2; Wang, Yongqiang 1,2; Zhao, Yue 1,2; She, Ruiping 1,2; Wang, Mei-Xiang 4; Wang, De-Xian 3; Tang, Jun 1,2
刊名	PLOS ONE
	2015-06-04
卷号	10 期号:6
英文摘要	Alternative chemo-reagents are in great demand because chemotherapy resistance is one of the major challenges in current cancer treatment. 5-hydoxy-1H-pyrrol-2-(5H)-one is an important N-heterocyclic scaffold that is present in natural products and medicinal chemistry. However, its antitumor activity has not been systematically explored. In this study, we screened a panel of 5-hydoxy-1H-pyrrol-2-(5H)-one derivatives and identified compound 1d as possessing strong anti-proliferative activity in multiple cancer cell lines. Cell cycle analysis revealed that 1d can induce S-phase cell cycle arrest and that HCT116 was sensitive to 1d-induced apoptosis. Further analysis indicated that 1d preferentially induced DNA damage and p53 activation in HCT116 cells and that 1d-induced apoptosis is partly dependent on p53. Furthermore, we showed that 1d significantly suppressed tumor growth in xenograft tumor models in vivo. Taken together, our results suggest that 5-hydoxy-1H-pyrrol-2-(5H)-one derivatives bear potential antitumor activity and that 1d is an effective agent for cancer treatment.
收录类别	SCI
语种	英语
公开日期	2015-11-02
内容类型	期刊论文
源URL	[http://ir.iccas.ac.cn/handle/121111/28178]
专题	化学研究所_分子识别与功能实验室
作者单位	1.China Agr Univ, State Key Lab Agrobiotechnol, Beijing 100193, Peoples R China 2.China Agr Univ, Coll Vet Med, Beijing 100193, Peoples R China 3.Chinese Acad Sci, Beijing Natl Lab Mol Sci, Inst Chem, CAS Key Lab Mol Recognit & Funct, Beijing 100190, Peoples R China 4.Tsinghua Univ, Dept Chem, Key Lab Bioorgan Phosphorus Chem & Chem Biol, Minist Educ, Beijing 100084, Peoples R China
推荐引用方式 GB/T 7714	Geng, Yunyun,Wang, Xiaojian,Yang, Luo,et al. Antitumor Activity of a 5-Hydroxy-1H-Pyrrol-2-(5H)-One-Based Synthetic Small Molecule In Vitro and In Vivo[J]. PLOS ONE,2015,10(6).
APA	Geng, Yunyun.,Wang, Xiaojian.,Yang, Luo.,Sun, Haili.,Wang, Yongqiang.,...&Tang, Jun.(2015).Antitumor Activity of a 5-Hydroxy-1H-Pyrrol-2-(5H)-One-Based Synthetic Small Molecule In Vitro and In Vivo.PLOS ONE,10(6).
MLA	Geng, Yunyun,et al."Antitumor Activity of a 5-Hydroxy-1H-Pyrrol-2-(5H)-One-Based Synthetic Small Molecule In Vitro and In Vivo".PLOS ONE 10.6(2015).