Discovery and structural modification of novel inhibitors of PTP1B inspired by the ACT fragment of scleritodermin A

被引：6

作者：

Wei, Yi ^{[1
]}

Chen, Yue-Ting ^{[1
]}

Shi, Lei ^{[1
]}

Gao, Li-Xin ^{[1
]}

Liu, Shen ^{[1
]}

Cui, Yong-Mei ^{[1
]}

Zhang, Wei ^{[1
]}

Shen, Qiang ^{[1
]}

Li, Jia ^{[1
]}

Nan, Fa-Jun ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Chinese Natl Ctr Drug Screening, Shanghai 201203, Peoples R China

来源：

MEDCHEMCOMM | 2011年 / 2卷 / 11期

基金：

中国国家自然科学基金;

关键词：

TYROSINE-PHOSPHATASE; 1B; DIVERSITY-ORIENTED SYNTHESIS; INSULIN SENSITIVITY; NATURAL-PRODUCTS; PROTEIN; MICE; INSPIRATION; DERIVATIVES; ADIPOSITY; CHEMISTRY;

D O I：

10.1039/c1md00153a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of compounds synthesized from a key intermediate in the total synthesis of Scleritodermin A containing a novel conjugated thiazole moiety, 2-(1-amino-2-p-hydroxyphenylethane)-4-(4-carboxy2,4-dimethyl-2Z,4E-propadiene)-thiazole (ACT), were discovered to be potent inhibitors of protein tyrosine phosphatase 1B, with IC(50) values in the low micromolar range. Structure-activity relationships around the scaffold were investigated and some compounds exhibited more potent PTP1B inhibitory activity and improved specificities compared with the original hit.

引用

页码：1104 / 1109

页数：6

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