Zhang, Dengyou published the artcileSynthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors, Application of 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one, the publication is Bioorganic & Medicinal Chemistry (2013), 21(21), 6804-6820, database is CAplus and MEDLINE.
A series of 2-amino-N-benzylpyridine-3-carboxamides, 2-amino-N-benzylpyridine-3-sulfonamides and 2-amino-3-benzylthiopyridines against c-Met were designed by means of bioisosteric replacement and docking anal. Optimization of the 2-amino-3-benzylthiopyridine scaffold led to the identification of compound I displaying c-Met inhibition with an IC50 up to 7.7 nM. In the cytotoxic evaluation, compound I effectively inhibited the proliferation of c-Met addictive human cancer cell lines (IC50 from 0.19 to 0.71 μM) and c-Met activation-mediated cell metastasis. At a dose of 100 mg/Hg, I evidently inhibited tumor growth (45%) in NIH-3T3/TPR-Met xenograft model. Of note, I could overcome c-Met-activation mediated gefitinib-resistance, which indicated its potential use for drug combination. Taken together, 2-amino-3-benzylthiopyridine scaffold was first disclosed and exhibited promising pharmacol. profiles against c-Met, which left room for further exploration.
Bioorganic & Medicinal Chemistry published new progress about 837392-64-0. 837392-64-0 belongs to indole-building-block, auxiliary class Indoline,Boronic acid and ester,Amide,Boronate Esters, name is 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one, and the molecular formula is C17H29BO2, Application of 5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)indolin-2-one.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles