647858-40-0

Upstream product

• 403-19-0 2-fluoro-4-nitrophenol 
• 647858-19-3 2-(2-fluoro-4-nitrophenoxy)ethan-1-ol 
• 110-89-4 piperidine 
• 647858-37-5 methanesulfonic acid 2-(2-fluoro-4-nitro-phenoxy)-ethyl ester 

Downstream Products

• 647858-46-6 (R)-5-Azidomethyl-3-[3-fluoro-4-(2-piperidin-1-yl-ethoxy)-phenyl]-oxazolidin-2-one 
• 647858-49-9 (S)-5-Aminomethyl-3-[3-fluoro-4-(2-piperidin-1-yl-ethoxy)-phenyl]-oxazolidin-2-one 
• 647858-43-3 (R)-3-[3-Fluoro-4-(2-piperidin-1-yl-ethoxy)-phenyl]-5-hydroxymethyl-oxazolidin-2-one 
• 851597-46-1 3-fluoro-4-{[2-(1-piperidinyl)ethyl]oxy}aniline 

Relevant academic research and scientific papers

Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: Design, synthesis and 3D-QSAR studies

VEGFR-2 plays an essential role in angiogenesis and is a central target for anticancer drug discovery. In order to develop novel VEGFR-2 inhibitors, we designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds (18b, 20e, 20h and 20j) are potent VEGFR-2 inhibitors which are comparable to positive control. Compound 18b displayed the most potent VEGFR-2 inhibition with IC50 value of 2.02 nM. Moreover, it exhibited promising antiproliferative activity against MCF-7 and SMMC-7721 cells with IC50 values of 1.47 μM and 5.98 μM, respectively. Molecular docking and 3D-QSAR studies were also carried out. The results indicated that these biphenyl amides could serve as promising leads for further optimization as novel VEGFR-2 inhibitors.

2-Pyrimidinyl Pyrazolopyridine Erbb Kinase Inhibitors

The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.

Influence of ethylene-oxy spacer group on the activity of linezolid: Synthesis of potent antibacterials possessing a thiocarbonyl group

The influence of an ethylene-oxy spacer element between the heterocycle and the aromatic ring in linezolid is reported. The introduction of such spacer group generated compounds with inferior antibacterial activity. However, the conversion of the acetamide group present in the linezolid analogues to either thiocarbamate or thioacetamide functionality restored the activity. The synthesis of linezolid analogues possessing the ethylene-oxy spacer group along with SAR studies with different heterocycles and preparation of some thiocarbonyl compounds possessing potent antibacterial property are presented.