Li, Chunpu published the artcileDesign, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, the publication is ACS Medicinal Chemistry Letters (2015), 6(5), 507-512, database is CAplus and MEDLINE.
A series of imidazo[1,2-a]pyridine derivatives against c-Met was designed by means of bioisosteric replacement. In this study, a selective, potent c-Met inhibitor, I was identified, with IC50 values of 3.9 nM against c-Met kinase and 45.0 nM against c-Met-addicted EBC-1 cell proliferation, resp. Compound I inhibited c-Met phosphorylation and downstream signaling across different oncogenic forms in c-Met overactivated cancer cells and model cells. Compound I significantly inhibited tumor growth (TGI = 75%) with good oral bioavailability (F = 29%) and no significant hERG inhibition. On the basis of systematic metabolic study, the pathway of all possible metabolites of I in liver microsomes of different species has been proposed, and a major NADPH-dependent metabolite was generated by liver microsomes. To block the metabolic site, II was designed and synthesized for further evaluation. Taken together, the imidazo[1,2-a]pyridine scaffold showed promising pharmacol. inhibition of c-Met and warrants further investigation.
ACS Medicinal Chemistry Letters published new progress about 1190875-39-8. 1190875-39-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Piperidine,Boronic acid and ester,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid, and the molecular formula is C13H22BN3O4, Recommanded Product: (1-(1-(tert-Butoxycarbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)boronic acid.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
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