Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase
نویسندگان
چکیده
منابع مشابه
Synthesis and Evaluation of Ethyl 2,4-dioxo-4-arylbutanoate Derivatives as Src Kinase Inhibitors
In this work, different ethyl 2,4-dioxo-4-arylbutanoate derivatives were prepared and evaluated for their Src Kinase inhibitory activity. For this purpose, the appropriate substituted acetophenone derivatives reacted with diethyl oxalate in the presence of sodium ethoxide in dried ethanol to give the corresponding products. All compounds showed moderate activities comparing with staurosporine a...
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Stringent regulation of tyrosine kinase activity is essential for normal cellular function. In humans, the tyrosine kinase Src is inhibited via phosphorylation of its C-terminal tail by another kinase, C-terminal Src kinase (Csk). Although Src and Csk orthologs are present across holozoan organisms, including animals and protists, the Csk-Src negative regulatory mechanism appears to have evolve...
متن کاملControl of excitatory synaptic transmission by C-terminal Src kinase.
The induction of long-term potentiation at CA3-CA1 synapses is caused by an N-methyl-d-aspartate (NMDA) receptordependent accumulation of intracellular Ca(2+), followed by Src family kinase activation and a positive feedback enhancement of NMDA receptors (NMDARs). Nevertheless, the amplitude of baseline transmission remains remarkably constant even though low frequency stimulation is also assoc...
متن کاملsynthesis and evaluation of ethyl 2,4-dioxo-4-arylbutanoate derivatives as src kinase inhibitors
in this work, different ethyl 2,4-dioxo-4-arylbutanoate derivatives were prepared and evaluated for their src kinase inhibitory activity. for this purpose, the appropriate substituted acetophenone derivatives reacted with diethyl oxalate in the presence of sodium ethoxide in dried ethanol to give the corresponding products. all compounds showed moderate activities comparing with staurosporine a...
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Pragmin is one of the few mammalian proteins containing the Glu-Pro-Ile-Tyr-Ala (EPIYA) tyrosine-phosphorylation motif that was originally discovered in the Helicobacter pylori CagA oncoprotein. Following delivery into gastric epithelial cells by type IV secretion and subsequent tyrosine phosphorylation at the EPIYA motifs, CagA serves as an oncogenic scaffold/adaptor that promiscuously interac...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2019
ISSN: 1948-5875,1948-5875
DOI: 10.1021/acsmedchemlett.9b00354