The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: tert-Butyl 2-cyanoacetate( cas:1116-98-9 ) is researched.Recommanded Product: tert-Butyl 2-cyanoacetate.Mostinski, Yelena; Heynen, Guus J. J. E.; Lopez-Alberca, Maria Pascual; Paul, Jerome; Miksche, Sandra; Radetzki, Silke; Schaller, David; Shanina, Elena; Seyffarth, Carola; Kolomeets, Yuliya; Ziebart, Nandor; de Schryver, Judith; Oestreich, Sylvia; Neuenschwander, Martin; Roske, Yvette; Heinemann, Udo; Rademacher, Christoph; Volkamer, Andrea; von Kries, Jens Peter; Birchmeier, Walter; Nazare, Marc published the article 《From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement》 about this compound( cas:1116-98-9 ) in Journal of Medicinal Chemistry. Keywords: azaindole SHP2 inhibitor synthesis anticancer drug resistance tumor relapse. Let’s learn more about this compound (cas:1116-98-9).
The tyrosine phosphatase SHP2 controls the activity of pivotal signaling pathways, including MAPK, JAK-STAT, and PI3K-Akt. Aberrant SHP2 activity leads to uncontrolled cell proliferation, tumorigenesis, and metastasis. SHP2 signaling was recently linked to drug resistance against cancer medications such as MEK and BRAF inhibitors. In this work, we present the development of a novel class of azaindole SHP2 inhibitors. We applied scaffold hopping and bioisosteric replacement concepts to eliminate unwanted structural motifs and to improve the inhibitor characteristics of the previously reported pyrazolone SHP2 inhibitors. The most potent azaindole I inhibits SHP2 with an IC50 = 0.031μM in an enzymic assay and with an IC50 = 2.6μM in human pancreas cells (HPAF-II). Evaluation in a series of cellular assays for metastasis and drug resistance demonstrated efficient SHP2 blockade. Finally, I inhibited proliferation of two cancer cell lines that are resistant to cancer drugs and diminished ERK signaling.
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Reference:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem