67988-50-5Relevant academic research and scientific papers
IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS
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, (2020/06/05)
The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.
A 2, 7-naphthyridine-based fluorescent turn-on probe for detection of biothiols in vitro and in vivo
Cao, Yun-Feng,Dong, Huan,Luo, Xiao-Gang,Peng, Hong-Tao,Ren, Rui,She, Neng-Fang,Sun, Qi,Wu, Pan-Pan,Zhuo, Lin-Sheng
, (2020/08/06)
A 2,7-naphthyridine derivative (AND-OH) was used as a fluorophore in the development of a novel fluorescent turn-on probe (AND-DNBS) by introducing a 2,4-dinitrobenzenesulfonate functionality. This fluorescent probe was successfully used for sensing glutathione (GSH) in aqueous media and showed favorable properties such as a rapid response time (45 s) and a significant Stokes shift (227 nm). The characteristics of the developed probe are better than those of another probe, namely ND-DNBS, which was also synthesized by our group and most other previously reported fluorescent probes for GSH. The AND-DNBS probe was able to detect GSH via a red emission in living A549 cells and zebrafishes. These results show that AND-DNBS has potential applications as an excellent probe for detecting GSH in various environments.
In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors
Tasker, Nikhil R.,Rastelli, Ettore J.,Blanco, Isabella K.,Burnett, James C.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
, p. 2448 - 2466 (2019/03/06)
A continuous flow photooxygenation of 7-aminothieno[3,2-c]pyridin-4(5H)-ones to produce 7-iminothieno[3,2-c]pyridine-4,6(5H,7H)-diones has been developed, utilizing ambient air as the sole reactant. N-H Imines are formed as the major products, and excellent functional group tolerance and conversion on gram-scale without the need for chromatographic purification allow for facile late-stage diversification of the aminothienopyridinone scaffold. Several analogs exhibit potent in vitro inhibition of the cancer-associated protein tyrosine phosphatase PTP4A3, and the SAR supports an exploratory docking model.
PYRIDINE DERIVATIVES, METHODS OF THEIR PREPARATIONS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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, (2010/11/24)
The present invention relates to pyridine derivatives having inhibitory effects on synthesis of cytokines, which are involved in inflammatory reactions, thus being useful as a therapeutic agent for treatment of inflammation-related diseases, immune-related diseases and chronic inflammatory diseases methods as well as an anti-inflammatory and analgesic agent, methods for their preparations, and pharmaceutical compositions containing the same.
