54608-35-4

Upstream product

• 103-63-9 1-phenyl-2-bromoethane 
• 459-73-4 GlyOEt*HCl 
• 623-33-6 glycine ethyl ester hydrochloride 
• 924-44-7 glyoxylic acid ethyl ester 
• 64-04-0 phenethylamine 
• 623-73-4 diazoacetic acid ethyl ester 
• 105-36-2 ethyl bromoacetate 
• 122-78-1 phenylacetaldehyde 

Downstream Products

• 856702-35-7 ethyl N'-(tert-butoxycarbonyl)glycyl-N-(2-phenylethyl)glycinate 
• 856702-32-4 ethyl N'-(tert-butoxycarbonyl)-L-valyl-N-(2-phenylethyl)glycinate 
• 54608-34-3 1-carbethoxymethyl-1-phenethylurea 
• 119811-30-2 N-benzenesulfonyl-N-phenethyl-glycine 
• 1223389-60-3 ethyl (allyloxycarbonyl-(2-phenethyl)amino)acetate 
• 1375092-49-1 C₁₈H₂₅NO₂ 
• 949902-88-9 (2-hydroxyethyl)phenethylcarbamic acid t-butyl ester 
• 182921-00-2 (2-oxoethyl)phenethylcarbamic acid t-butyl ester 
• 193818-10-9 (t-butoxycarbonylphenethylamino)acetic acid ethyl ester 
• 1332457-48-3 ethyl 2-(N-phenethylacetamido)acetate 

Relevant academic research and scientific papers

Psammocindoles A-C: Isolation, Synthesis, and Bioactivity of Indole-γ-lactams from the Sponge Psammocinia vermis

Psammocindoles A-C (1-3), a new class of indole alkaloids, were isolated from a Psammocinia vermis sponge. By combined spectroscopic analyses, the structures of these compounds were determined to be the indole-γ-lactams derived from three amino acid residues. In addition, an enantiomer psammocindole D (4), and the N-lactam isomers isopsammocindoles A-D (5-8) were also synthesized. These natural products and synthetic analogues were found to significantly stimulate adiponectin secretion in human bone marrow mesenchymal stem cells.

Optimization and SAR investigation of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as EGFR and BRAFV600E dual inhibitors with potent antiproliferative and antioxidant activities

Using a single drug to treat cancer with dual-targeting is an unusual approach when compared to other drug combinations. Dual-targeting agents were developed as a result of insufficient efficacy and drug resistance when single-targeting agents were used.

EIF4E INHIBITORS AND USES THEREOF

The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.

Design and synthesis of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as antiproliferative EGFR and BRAFV600E dual inhibitors

Recent studies have shown additive and synergistic effects associated with the combination of kinase inhibitors. BRAFV600E and EGFR are attractive targets for many diseases treatments and have been studied extensively. In keeping with our interest in developing anticancer targeting EGFR and BRAFV600E, a novel series of 2,3-dihydropyrazino[1,2-a]indole-1,4-dione has been rationally designed, synthesized and evaluated for their antiproliferative activity against a panel of four human cancer cell lines. Compounds 20–23, 28–31, and 33 showed promising antiproliferative activities. These compounds were further tested for their inhibitory potencies against EGFR and BRAFV600E kinases with erlotinib as a reference drug. Compounds 23 and 33 exhibited equipotency to doxorubicin against the four cell lines and efficiently inhibited both EGFR (IC50 = 0.08 and 0.09 μM, respectively) and BRAFV600E (IC50 = 0.1 and 0.29 μM, respectively). In cell cycle study of MCF-7 cell line, compounds 23 and 33 induced apoptosis and exhibited cell cycle arrest in both Pre-G1 and G2/M phases. Molecular docking analyses revealed that the new compounds can fit snugly into the active sites of EGFR, and BRAFV600E kinases. Compound 23, 31 and 33 adopted similar binding orientations and interactions to those of erlotinib and vemurafenib.

The discovery of new human coagulation factor XIa (FXIa) inhibitors by synthesis, biological evaluation, and structure-based modeling

Factor XIa (FXIa) is an enzyme that is activated during the earliest stage of initiation of the intrinsic pathway of the blood coagulation mechanism. In this study, we attempted to discover a new FXIa inhibitor based on structure-based molecular modeling. We found that compound 16 exhibits satisfactory predicted properties while maintaining important binding interactions with FX1a.

Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1

Eukaryotic mRNA contains a 3′ poly(A) tail, which plays important roles in the regulation of mRNA stability and translation. Well-characterized enzymes involved in the shortening of the poly(A) tail include the multi-subunit Ccr4-Not deadenylase, which contains the Caf1 (Pop2) and Ccr4 catalytic components, and poly(A)-specific ribonuclease (PARN). Two Mg2+ ions present in the active sites of these ribonucleases are required for RNA cleavage. Here, we report the discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as (sub)micromolar inhibitors of Caf1.

New Compound Having Inhibition Activity to Factor XIa

The present invention relates to a pharmacologically active amount of a novel compound, represented by chemical formula 1, having inhibition activity against factor XIa, a producing method thereof, and a pharmaceutical composition comprising: a pharmaceut

Frequency of C-allylations on oligoglycinates via N-ylides

The highly selective mono-C-allylation of oligoglycinates such as a diethylenetriaminepentaacetate, an iminodiacetate, and an ethylenediaminetetraacetate via insertion of a vacuum operation between the N-allylation and C-migration steps is reported. It is contrastive that one-pot N-allylation-C-allylation procedure gave a mixture including multiallylated products. In the reaction with N-ylides, gem-C-diallylation and α,α′-C-diallylation of oligoglycinates are strongly inhibited even with the use of an excess of allyl bromide and base. A mechanism to explain this control of the frequency of C-allylation on oligoglycinates via N-ylides is also proposed.

Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics

The neurotensin receptor subtype 2 (NTS2) is involved in the modulation of tonic pain sensitivity and psychiatric diseases and is, therefore, regarded as a highly attractive pharmacological target protein. Aiming to discover NTS2 selective ligands, we her

Leccinine A, an endoplasmic reticulum stress-suppressive compound from the edible mushroom Leccinum extremiorientale

Leccinine A (1) along with a known compound (2), were isolated from the edible mushroom Leccinum extremiorientale. The structure of 1 was determined by the interpretation of spectral data. Leccinine A showed protective activity against endoplasmic reticulum stress-dependent cell death. Seven analogues (3-9) of 1 were synthesized in order to evaluate the structure-activity relationship, and the result indicated that the formamide group of 1 was indispensable for the activity.