Synthesis and Biological Activities of Novel 2,5-Disubstituted-1,3,4-thiadiazole Derivatives

doi:10.6023/cjoc201405020

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	Synthesis and Biological Activities of Novel 2,5-Disubstituted-1,3,4-thiadiazole Derivatives
	Li Yingjun 1; Yu Yang 1; Jin Kun 2; Gao Lixin 3; Luo Tongchuan 1; Sheng Li 3; Shao Xin 1; Li Jia3
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2015-01
卷号	35 期号:1 页码:129-136
关键词	2,5-disubstituted-1,3,4-thiadiazole benzisoselenazolone synthesis bioactivity
ISSN号	0253-2786
DOI	10.6023/cjoc201405020
文献子类	Article
英文摘要	Sixteen novel 2,5-disubstituted-1,3,4-thiadiazole derivatives containing benzisoselenazolone moiety 7a similar to 7p were synthesized by the reaction of 2-amino-5-substituted-1,3,4-thiadiazoles (2) with ortho-(chloroseleno)benzoyl chloride (6). The structures were characterized by IR, H-1 NMR spectra and elemental analysis. Their biological activities were evaluated. The experimental results indicate that some compounds exhibit inhibitory activity against cell division cycle 25B phosphatase (Cdc25B) (IC50 = 1.67 similar to 6.66 mu mol.L-1). All the target compounds showed good inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) (IC50 =-0.73 similar to 4.50 mu mol.L-1), and some compounds exhibited higher inhibitory activity than positive control oleanolic acid (IC50= 1.90 mu mol.L-1). Compound 7k displayed antitumor activity in vitro for human colon cancer (HCT-8) cell (IC50= 12.54 mu mol.L-1). Some compounds showed the medium scavenging ability for hydroxyl radical (HO center dot) and superoxide anion (O-2(center dot-)), but no scavenging ability for DPPH center dot.
资助项目	Natural Science Foundation of Liaoning Province[20102126]
WOS关键词	INHIBITORS ; POTENT ; HETEROCYCLE ; AGONISTS ; SERIES ; AGENTS
WOS研究方向	Chemistry
语种	中文
CSCD记录号	CSCD:5353193
出版者	SCIENCE PRESS
WOS记录号	WOS:000351191700012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276738]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室药物安全性评价中心
通讯作者	Li Yingjun
作者单位	1.Liaoning Normal Univ, Coll Chem & Chem Engn, Dalian 116029, Peoples R China; 2.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116012, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Li Yingjun,Yu Yang,Jin Kun,et al. Synthesis and Biological Activities of Novel 2,5-Disubstituted-1,3,4-thiadiazole Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2015,35(1):129-136.
APA	Li Yingjun.,Yu Yang.,Jin Kun.,Gao Lixin.,Luo Tongchuan.,...&Li Jia.(2015).Synthesis and Biological Activities of Novel 2,5-Disubstituted-1,3,4-thiadiazole Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,35(1),129-136.
MLA	Li Yingjun,et al."Synthesis and Biological Activities of Novel 2,5-Disubstituted-1,3,4-thiadiazole Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 35.1(2015):129-136.