142770-29-4Relevant academic research and scientific papers
A kind of benzene ring - aromatic ring series compound, its preparation method and medical use
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Paragraph 0146; 0149, (2017/12/05)
The invention relates to a phenyl ring-aromatic ring cascaded micro-molecular organic compound which can be used as a protein-tyrosine-phosphatase subtype inhibitor and is shown in a general formula I as described in the specification. The compound can be used as a tool compound for research on the biological functions of a variety of subtypes of a protein-tyrosine-phosphatase family in cell signal transduction, so novel means is provided for prevention and treatment of cancers, metabolism and immunological diseases, cardiovascular diseases and nervous diseases. The invention also relates to a preparation method and medicinal application of the compound.
Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors
Wang, Wen-Long,Huang, Chao,Gao, Li-Xin,Tang, Chun-Lan,Wang, Jun-Qing,Wu, Min-Chen,Sheng, Li,Chen, Hai-Jun,Nan, Fa-Jun,Li, Jing-Ya,Li, Jia,Feng, Bainian
supporting information, p. 1889 - 1894 (2014/04/17)
A series of bis-aromatic amides was designed, synthesized, and evaluated as a new class of inhibitors with IC50 values in the micromolar range against protein tyrosine phosphatase 1B (PTP1B). Among them, compound 15 displayed an IC50 value of 2.34 ± 0.08 μM with 5-fold preference over TCPTP. More importantly, the treatment of CHO/HIR cells with compound 15 resulted in increased phosphorylation of insulin receptor (IR), which suggested extensive cellular activity of compound 15. These results provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Synthesis of analogues of Congo red and evaluation of their anti-prion activity
Sellarajah, Shane,Lekishvili, Tamuna,Bowring, Claire,Thompsett, Andrew R.,Rudyk, Helene,Birkett, Christopher R.,Brown, David R.,Gilbert, Ian H.
, p. 5515 - 5534 (2007/10/03)
No cure as of yet exists for any of the transmissible spongiform encephalopathies. In this paper, we describe the synthesis of analogues of Congo red and evaluation against a cellular model of infection, the SMB (scrapie mouse brain) persistently infected cell line, for their ability to inhibit the infectivity of the abnormal form of prion protein (PrP-res). The compounds have also been tested for their ability to inhibit the polymerization of PrP C by PrP-res. A number of analogues showed inhibition of PrP-res infectivity at nanomolar concentrations. Several analogues show promise; the most active compound, 2a, inhibits the formation of PrP-res in SMB cells with an EC50 of 25-50 nM.
