新型25二取代134噻二唑衍生物的合成与生物活性

doi:10.6023/cjoc201405020

	新型25二取代134噻二唑衍生物的合成与生物活性
	李英俊 1; 于洋 1; 靳焜 2; 高立信 3; 罗潼川 1; 盛丽 3; 邵昕 1; 李佳 3
刊名	有机化学
	2015
卷号	35 期号:1 页码:129
关键词	INHIBITORS HETEROCYCLE SERIES AGENTS 2,5-disubstituted-1,3,4-thiadiazole benzisoselenazolone synthesis bioactivity
ISSN号	0253-2786
DOI	10.6023/cjoc201405020
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]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/284066]
专题	中国科学院上海药物研究所
作者单位	1.辽宁师范大学 2.大连理工大学 3.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	李英俊,于洋,靳焜,等. 新型25二取代134噻二唑衍生物的合成与生物活性[J]. 有机化学,2015,35(1):129.
APA	李英俊.,于洋.,靳焜.,高立信.,罗潼川.,...&李佳.(2015).新型25二取代134噻二唑衍生物的合成与生物活性.有机化学,35(1),129.
MLA	李英俊,et al."新型25二取代134噻二唑衍生物的合成与生物活性".有机化学 35.1(2015):129.