32150-92-8

Upstream product

• 85-44-9 phthalic anhydride 
• 673-06-3 D-(R)-phenylalanine 
• 63-91-2 L-phenylalanine 
• 3588-64-5 2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionic acid 
• 673-06-3 D-β-Phenyl-α-alanine 
• 3588-64-5 phthalyl-L-phenylalanine 
• 63-91-2 L-phenylalanine 

Downstream Products

• 155975-17-0 N,N-phthaloyl-D-phenylalanin-anilide 
• 111978-68-8 N,N-phthaloyl-D-phenylalanine-butyl ester 
• 131232-39-8 N,N-phthaloyl-D-phenylalanine nitrile 
• 142597-24-8 1-[(R)-2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionyl]-1H-pyrrole-2-carbaldehyde 
• 166734-67-4 (R)-2-phthalimido-3-phenylpropionaldehyde 
• 866395-47-3 (R)-1-diazo-3-phthalimido-4-phenylbutan-2-one 
• 16876-72-5 (R)-2-amino-N,3-diphenyl-propanamide 

Relevant academic research and scientific papers

NOVEL TRF1 MODULATORS AND ANALOGUES THEREOF

Novel TRF1 modulators and analogues thereof. There is provided compounds of Formula I, wherein R, R1, R2 and X have meanings written in the description. Such compounds are useful as TRF1 inhibitors and, for that reason, as medicaments, in the treatment of cancer, particularly high cancer stem cell cancer like glioblastoma and lung cancer, and can be also useful for the development of additional TRF1 inhibitors and increasing knowledge about TRF1 activity.

AMINO ACID DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES

The present disclosure provides certain amino acid derivatives that inhibit NF-kB activation and are therefore useful for the treatment of inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Oximino naphthoquinone compound and preparation and application methods thereof

The invention belongs to the technical field of medicinal compounds and medicines and relates to an oximino naphthoquinone compound and preparation and application methods thereof, particularly to a compound shown as formula (I). The oximino naphthoquinone compound can serve as a double-target selective inhibitor of STAT3 (signal transducer and activator of transcription-3) and IDO1 (indoleamine 2, 3-dioxygenase 1) for treating ovarian cancer, colon cancer, lung cancer and the like.

Flupirtine and retigabine as templates for ligand-based drug design of KV7.2/3 activators

Drug induced liver injury (DILI) and tissue discoloration led to the recent discontinuation of the therapeutic use of the closely related drugs flupirtine and retigabine, respectively. Experience gained with these drugs strongly suggests that heterotetramer, voltage-gated potassium channels 2 and 3 (KV7.2/3) are valid targets for effective treatment of pain and epilepsy. Because the adverse effects are not related to the mechanism of action, it appears promising to investigate chemical modifications of these clinically validated, drug-like leads. In the present retro-metabolic drug design study, a series of 43 compounds were synthesized and characterized with regard to KV7.2/3 opening activity and efficacy. The most active compound 22d displays excellent potency (EC50 = 4 nM) and efficacy (154%) as a KV7.2/3 opener. Limited aqueous solubility hampered toxicity testing at concentrations higher than 63 μM, but this concentration was nontoxic to two hepatocellular cell lines (HEP-G2 and TAMH) in culture. The slightly less active but more soluble compound 25b (EC50 = 11 nM, efficacy 111%) showed an improved toxicity/activity ratio compared to flupirtine by three orders of magnitude and represents an attractive lead structure for the development of safer analgesics and antiepileptics.

Structure-driven design and synthesis of chiral dioxocyclam derivatives

Based on an analysis of previously reported structures and a potential geometry fit with substrates, a new family of chiral dioxocyclam derivatives have been designed. The synthesis of those ligands was accomplished starting from l-proline and α-d-amino acids (converted to β-amino acids) with a key step of macrocyclization reaction of amino esters. All ligands were converted into neutral copper(II) complexes (amide groups underwent deprotonation of upon treatment of ligands with copper(II) acetate). The complexes exhibit the desired shape of their active surfaces, as proved by X-ray analysis.

Synthesis and Amino Acid Chain Extension of 1-Acylated Hydroxymethylpyrroles

Acylation of pyrrole-2-carbaldehyde (3) with an N-phthaloyl amino acid chloride, N,N-diisopropylethylamine and 4-dimethylaminopyridine (dmap) gave the 1-acylpyrrole-2-carbaldehydes (4a-c).The 1-acylated pyrroles (4d-i), (8) and (9) were similarly prepared

SULFUR YLIDES. 3. SYNTHESIS OF KETO-GROUP STABILIZED AMINO-CONTAINING SULFUR YLIDES FROM AMINO ACIDS

An effective path of synthesis was developed of new synthetic intermediates, the optically active, keto-group stabilized amino-substituted sulfur ylides.