Synthesis of 5-Phenyl-1,3,4-thiadiazole Derivatives and Their Biochemical Evaluation against Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase 1 (SHP1)

doi:10.6023/cjoc202104041

	Synthesis of 5-Phenyl-1,3,4-thiadiazole Derivatives and Their Biochemical Evaluation against Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase 1 (SHP1)
	Yu Lijie 2; Feng Bo 1,3,4; Wang Zhijia 2; Gao Lixin 2,3; Zhang Chun 2,5; Rajendran, Satheeshkumar 2; Li Jia 3; Zhou Yubo 1,3,4; Wang Wenlong 2
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2021-08-25
卷号	41 期号:8 页码:3097-3105
关键词	5-phenyl-1,3,4-thiadiazole derivatives Src homology 2 domain-containing protein tyrosine phosphatase 1 (SHP1) inhibitors structure-activity relationships
ISSN号	0253-2786
DOI	10.6023/cjoc202104041
通讯作者	Zhou Yubo(ybzhou@simm.ac.cn) ; Wang Wenlong(wwenlong2011@163.com)
英文摘要	The Src homology 2 domain-containing protein tyrosine phosphatase 1 (SHP1) is a convergent node for oncogenic cell-signaling cascades. Consequently, SHP1 represents a potential target for drug development in cancer treatment. Meanwhile only countable SHP1 inhibitors have been reported. A new type of SHP1 inhibitors with 5-phenyl-1,3,4-thiadiazole scaffold was developed. The representative compound 5b exhibited SHP1 inhibitory activity with IC50 of (1.33 +/- 0.16) mu mol/L, exhibited about 2-fold selectivity for SHP1 over SHP2, and had no detectable activity against PTP1B and TCPTP, and offered a novel scaffold to develop new SHP1 inhibitors.
资助项目	National Natural Science Foundation of China[21772068] ; National Natural Science Foundation of China[81773779] ; Postgraduate Research & Practice Innovation Program of Jiangsu Province[KYCX20-1965] ; Natural Science Foundation of Jiangsu Province[BK20190608]
WOS关键词	BIOLOGICAL EVALUATION ; INHIBITORS ; SPECIFICITY ; SUBSTRATE ; PTP1B
WOS研究方向	Chemistry
语种	英语
出版者	SCIENCE PRESS
WOS记录号	WOS:000702991300013
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297499]
专题	中国科学院上海药物研究所
通讯作者	Zhou Yubo; Wang Wenlong
作者单位	1.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Inst Drug Discovery, Zhongshan 528400, Guangdong, Peoples R China 2.Jiangnan Univ, Sch Pharmaceut Sci, Wuxi 214122, Jiangsu, Peoples R China 3.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Inst Dev, Zhongshan 528400, Guangdong, Peoples R China 5.Nanjing Univ, Sch Chem & Chem Engn, Nanjing 210023, Peoples R China
推荐引用方式 GB/T 7714	Yu Lijie,Feng Bo,Wang Zhijia,et al. Synthesis of 5-Phenyl-1,3,4-thiadiazole Derivatives and Their Biochemical Evaluation against Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase 1 (SHP1)[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2021,41(8):3097-3105.
APA	Yu Lijie.,Feng Bo.,Wang Zhijia.,Gao Lixin.,Zhang Chun.,...&Wang Wenlong.(2021).Synthesis of 5-Phenyl-1,3,4-thiadiazole Derivatives and Their Biochemical Evaluation against Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase 1 (SHP1).CHINESE JOURNAL OF ORGANIC CHEMISTRY,41(8),3097-3105.
MLA	Yu Lijie,et al."Synthesis of 5-Phenyl-1,3,4-thiadiazole Derivatives and Their Biochemical Evaluation against Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase 1 (SHP1)".CHINESE JOURNAL OF ORGANIC CHEMISTRY 41.8(2021):3097-3105.