synthesisofaromaticamidederivativesandtheirbiologicalevaluationagainstproteintyrosinephosphatase1bandscrhomology2domaincontainingproteintyrosinephosphatase2

doi:10.6023/cjoc201603045

	synthesisofaromaticamidederivativesandtheirbiologicalevaluationagainstproteintyrosinephosphatase1bandscrhomology2domaincontainingproteintyrosinephosphatase2
	Wang WL(王文龙)1; Luo H(骆欢)1; Gao Y(高雅)1; Gao LX(高立信)2; Sheng L(盛丽)2; Zhou YB(周宇波)2; Li J(李佳)2; Li JY(李静雅)2; Feng BN(冯柏年)1
刊名	chinesejournaloforganicchemistry
	2016
卷号	36 期号:9 页码:2142
关键词	OLEANOLIC ACID INHIBITORS PTP1B PTP1B SHP2 aromatic amide derivatives inhibitors
ISSN号	0253-2786
DOI	10.6023/cjoc201603045
英文摘要	To explore the chemical space of protein tyrosine phosphatase 1B (PTP1B) inhibitors by changing bis-aromatic amide moiety into aromatic amide moiety, a series of aromatic amide derivatives were designed, synthesized and their biological activities were evaluated against PTP1B and Scr homology-2 domain containing protein tyrosine phosphatase-2 (SHP2). Among them, compound 3c displayed moderate inhibitory activity with IC50 of (5.13 +/- 0.21) mu mol/L against PTP1B and showed two times selectivity for other related PTPs. Interestingly, compound 12 IC50=(7.47 +/- 1.26) mu mol/L showed moderate inhibitory activity against SHP2 and 2-fold selectivity against PTP1B, T-cell protein tyrosine phosphatase (TCPTP) or Src homology-2 domain containing protein tyrosine phosphatase-1 (SHP1) respectively, and offered a novel scaffold to develop new SHP2 inhibitors.
资助项目	[National Natural Science Foundation of China] ; [State Key Laboratory of Drug Research]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/285873]
专题	中国科学院上海药物研究所
作者单位	1.江南大学 2.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Wang WL,Luo H,Gao Y,et al. synthesisofaromaticamidederivativesandtheirbiologicalevaluationagainstproteintyrosinephosphatase1bandscrhomology2domaincontainingproteintyrosinephosphatase2[J]. chinesejournaloforganicchemistry,2016,36(9):2142.
APA	王文龙.,骆欢.,高雅.,高立信.,盛丽.,...&冯柏年.(2016).synthesisofaromaticamidederivativesandtheirbiologicalevaluationagainstproteintyrosinephosphatase1bandscrhomology2domaincontainingproteintyrosinephosphatase2.chinesejournaloforganicchemistry,36(9),2142.
MLA	王文龙,et al."synthesisofaromaticamidederivativesandtheirbiologicalevaluationagainstproteintyrosinephosphatase1bandscrhomology2domaincontainingproteintyrosinephosphatase2".chinesejournaloforganicchemistry 36.9(2016):2142.