307330-12-7Relevant academic research and scientific papers
A class of 2, 3 - dihydronaphth block pyrimidine analogs, its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0185; 0187-0188, (2017/07/22)
The invention belongs to the technical field of medicines and relates to a 2,3-dihydronaphthalene-embedded m-diazabenzene analogue represented as the following general formula I and a preparation method thereof. The 2,3-dihydronaphthalene-embedded m-diazabenzene analogue has a function of inhibiting biological activities of different subtypes of a protein-tyrosine-phosphatase family (PTPases), can be used as a tool compound for researching a biological function correlation of the subtypes of the protein-tyrosine-phosphatase family (PTPases) in a cell signal transduction process, and provides a new approach for preventing and treating cancer, metabolic and immunological diseases, angiocardiopathy and neurological diseases.
1H-2,3-Dihydroperimidine derivatives: A new class of potent protein Tyrosine Phosphatase 1B inhibitors
Wang, Wen-Long,Yang, Dong-Lin,Gao, Li-Xin,Tang, Chun-Lan,Ma, Wei-Ping,Ye, Hui-Hua,Zhang, Si-Qi,Zhao, Ya-Nan,Xu, Hao-Jie,Hu, Zhao,Chen, Xia,Fan, Wen-Hua,Chen, Hai-Jun,Li, Jing-Ya,Nan, Fa-Jun,Li, Jia,Feng, Bainian
, p. 102 - 121 (2014/02/14)
A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
