869347-26-2

Upstream product

• 621-37-4 m-hydroxyphenylacetic acid 
• 75-03-6 ethyl iodide 
• 74-96-4 ethyl bromide 
• 22446-38-4 ethyl 3-hydroxyphenylacetate 

Downstream Products

• 328897-98-9 ethyl dimethyl-3-ethoxyphenylacetate 
• 869347-29-5 (+/-)-α-bromo-(3-ethoxyphenyl)acetic acid ethyl ester 
• 869347-39-7 (+/-)-α-ethyl-α-(3-ethoxyphenyl)-α-[[2-(1H-pyrrol-1-yl)phenyl]oxy]acetic acid ethyl ester 
• 869347-44-4 (+/-)-α-ethyl-α-(3-ethoxyphenyl)-α-[[2-(1H-pyrrol-1-yl)phenyl]oxy]acetic acid 
• 869347-34-2 (+/-)-α-(3-ethoxyphenyl)-α-[[2-(1H-pyrrol-1-yl)phenyl]oxy]acetic acid ethyl ester 

Relevant academic research and scientific papers

Fragment based discovery of arginine isosteres through REPLACE: Towards non-ATP competitive CDK inhibitors

In order to develop non-ATP competitive CDK2/cyclin A inhibitors, the REPLACE strategy has been applied to generate fragment alternatives for the N-terminal tetrapeptide of the cyclin binding motif (HAKRRLIF) involved in substrate recruitment prior to phosphotransfer. The docking approach used for the prediction of small molecule mimics for peptide determinants was validated through reproduction of experimental binding modes of known inhibitors and provides useful information for evaluating binding to protein-protein interaction sites. Further to this, potential arginine isosteres predicted using the validated LigandFit docking method were ligated to the truncated C-terminal peptide, RLIF using solid phase synthesis and evaluated in a competitive binding assay. After testing, identified fragments were shown to represent not only appropriate mimics for a critical arginine residue but also to interact effectively with a minor hydrophobic pocket present in the binding groove. Further evaluation of binding modes was undertaken to optimize the potency of these compounds. Through further application of the REPLACE strategy in this study, peptide-small molecule hybrid CDK2 inhibitors were identified that are more drug-like and suitable for further optimization as anti-tumor therapeutics.

SPHINGOSINE-1 -PHOSPHATE RECEPTOR AGONIST AND ANTAGONIST COMPOUNDS

The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity

Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT pro

NOVEL CIS-IMIDAZOLINES

Formula (I) and the pharmaceutically acceptable salts and esters thereof, wherein X1, X2, X3,Y1, Y2 and R are described herein inhibit the interaction of MDM2 protein with a p53-like peptide and hence have anti proiferative activity.