78756-28-2

Upstream product

• 75-44-5 phosgene 
• 55341-87-2 3-aminothiophene-2-carboxylic acid 
• 64615-13-0 3-Amino-2-thiophencarbonsaeure-methylester-hydrochlorid 
• 78756-27-1 sodium 3-aminothiophene-2-carboxylate 
• 71-36-3 butan-1-ol 
• 22288-78-4 Methyl 3-aminothiophene-2-carboxylate 
• 503-38-8 trichloromethyl chloroformate 
• 32315-10-9 bis(trichloromethyl) carbonate 
• 1210469-45-6 potassium 3-aminothiophene-2-carboxylate 
• 118235-61-3 3-ethoxycarbonylamino-thiophene-2-carboxylic acid 

Downstream Products

• 213390-51-3 3-(3-methylureido)thiophene-2-carboxylic acid 
• 213390-57-9 3-{[(benzyloxy)carbonyl]amino}thiophene-2-carboxylic acid 
• 231630-04-9 1-benzyl-2H-thieno[3,2-d][1,3]oxazine-2,4(1H)-dione 
• 934602-35-4 (S)-2-[(3-aminothiophene-2-carbonyl)amino]propionic acid 
• 934602-36-5 (S)-3-[3-(1-carboxyethyl)ureido]thiophene-2-carboxylic acid 
• 231630-06-1 3-(benzylamino)thiophene-2-carbonyl azide 
• 158460-93-6 [3-(4-Bromo-2-fluoro-benzyl)-6-chloro-2,4-dioxo-3,4-dihydro-2H-thieno[3,2-d]pyrimidin-1-yl]-acetic acid ethyl ester 
• 1086383-61-0 1-(4-methoxybenzyl)-1H-thieno[3,2-d][1,3]oxazine-2,4-dione 
• 686266-52-4 1-benzyl-7-methyl-2H-thieno[3,2-d][1,3]oxazine-2,4(1H)-dione 
• 103979-63-1 1-(3,4-Dimethoxy-phenyl)-3-(3-methylamino-thiophen-2-yl)-propane-1,3-dione 

Relevant academic research and scientific papers

IL4I1 INHIBITORS AND METHODS OF USE

Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.

Exploring the chemical space of ureidothiophene-2-carboxylic acids as inhibitors of the quorum sensing enzyme PqsD from Pseudomonas aeruginosa

Pseudomonas aeruginosa employs a quorum sensing (QS) communication system that makes use of small diffusible molecules. Among other effects, the QS system coordinates the formation of biofilm which decisively contributes to difficulties in the therapy of

PYRIDOPYRIMIDINEDIONE DERIVATIVES

The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.

Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents

A critical question in natural product-based drug discovery is how to translate the product into drug-like molecules with optimal pharmacological properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chemical space and identify promising drug leads. Extending our efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine (66c) showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound 66c is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery. (Figure Presented).

Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors

A series of thienopyridinone derivatives was designed and synthesized as inhibitors of checkpoint kinase 1 (Chk1). Most of them exhibited moderate to good Chk1 inhibitory activities. Among them, compounds 8q, 8t, and 8w with excellent Chk1 inhibitory activities (IC50 values of 4.05, 6.23, and 2.33 nM, respectively) displayed strong synergistic effects with melphalan, a DNA-damaging agent in the cell-based assay. Further kinase profiling indicated that compound 8t was highly selective against CDK2/cyclinA, Aurora A, and PKC.

NEW DS DNA BINDING FLUORESCENT DYES

The present invention is directed to a fluorescent dye comprising a benzothiazolium moiety and a pyrimidinium moiety connected by a mono-methine bridge, characterized in that (i) the 2-position of the pyrimidine carries a substituent which starts with a C

THIENOPYRIDINONE DERIVATIVES AS MACROPHAGE MIGRATION INHIBITORY FACTOR INHIBITORS

Inhibitors of macrophage migration inhibitory factor having a thienopyridinone backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with macrophage migration inhibitory factor activity. The inhibitors of macrophage migration inhibitory factor have the following structures formula (I), (II), (III) including forms such as stereoisomers, free forms, pharmaceutically acceptable salts or esters thereof, solvates, or combinations of such forms, wherein n, R1, R2, R3, X, and Y are as defined herein. Compositions comprising an inhibitor of macrophage migration inhibitory factor in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

THIENOPYRIDONE CARBOXAMIDES AND THEIR MEDICAL USE

A compound of formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C1-C4 alkyl, C1-C3 alkoxy; halogen, trifluoromethyl or OCHxFy, R′′ is hydrogen,

Anti-infective agents

Compounds having the formula are hepatitis C(HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C(HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Anti-infective agents

Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.