3223-20-9

Upstream product

• 96-97-9 5-nitrosalicylic acid 
• 69-72-7 salicylic acid 

Downstream Products

• 10515-56-7 2-hydroxy-5-nitro-benzoic acid-(2,4,6-trichloro-anilide) 
• 90765-78-9 2-hydroxy-5-nitro-N-thiazol-2-yl-benzamide 
• 65043-10-9 2-hydroxy-5-nitro-N-(2-oxo-oxazolidin-3-yl)-benzamide 
• 74688-65-6 N-(5-chloro-thiazol-2-yl)-2-hydroxy-5-nitro-benzamide 
• 74688-64-5 N-(5-bromo-thiazol-2-yl)-2-hydroxy-5-nitro-benzamide 
• 74688-66-7 2-(2-hydroxy-5-nitro-benzoylamino)-4-methyl-thiazole-5-carboxylic acid ethyl ester 
• 74675-85-7 N-[4-(4-chloro-phenyl)-thiazol-2-yl]-2-hydroxy-5-nitro-benzamide 
• 155388-68-4 2-Hydroxy-5-nitro-benzoic acid hexadecyl ester 
• 155388-70-8 2-hydroxy-5-nitrobenzoic acid 2-(1-tricyclo<3.3.1.1>decyl)ethyl ester 
• 6490-96-6 2-hydroxy-5-nitro-benzoic acid-(4-bromo-anilide) 
• 65043-12-1 2-Hydroxy-5-nitro-benzoyl Thiosemicarbazide 
• 68507-72-2 (2-hydroxy-5-nitrophenyl)(morpholino)methanone 
• 114259-81-3 (2-hydroxy-5-nitrophenyl)(4-methylpiperidin-1-yl)methanone 
• 68507-73-3 (2-hydroxy-5-nitrophenyl)(piperidin-1-yl)methanone 

Relevant academic research and scientific papers

Cathepsin B inhibitors: Further exploration of the nitroxoline core

Human cathepsin B is a cysteine protease with many house-keeping functions, such as intracellular proteolysis within lysosomes. Its increased activity and expression have been strongly associated with many pathological processes, including cancers. We present here the design and synthesis of novel derivatives of nitroxoline as inhibitors of cathepsin B. These were prepared either by omitting the pyridine part, or by modifying positions 2, 7, and 8 of nitroxoline. All compounds were evaluated for their ability to inhibit endopeptidase and exopeptidase activities of cathepsin B. For the most promising inhibitors, the ability to reduce extracellular and intracellular collagen IV degradation was determined, followed by their evaluation in cell-based in vitro models of tumor invasion. The presented data show that we have further defined the structural requirements for cathepsin B inhibition by nitroxoline derivatives and provided additional knowledge that could lead to non-peptidic compounds with usefulness against tumor progression.

Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

DNA-encoded chemical libraries are increasingly used to identify leads for drug discovery or chemical biology. Despite the resurging interest in covalent inhibitors, libraries are typically designed with synthon filtered out for reactive functionalities that can engage a target through covalent interactions. Herein, we report the synthesis of two libraries containing Michael acceptors to identify cysteine reactive ligands. We developed a simple procedure to discriminate between covalent and high affinity non-covalent inhibitors using DNA display of the library in a microarray format. The methodology was validated with known covalent and high affinity non-covalent kinase inhibitors. Screening of the library revealed novel covalent inhibitors for MEK2 and ERBB2.

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).

Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3Kγ

Phosphoinositide 3-kinase (PI3K) is an attractive target to potentially treat a range of disease states as illustrated by more than 15 inhibitors now in clinical trials. We disclose herein the discovery of a new class of fluoroquinolone derivatives having

N-BENZYLANILINE DERIVATIVE AND USES THEREOF

Disclosed are an N-benzylaniline derivative and uses thereof. The derivative is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound has an action of protecting against cerebral ischemia/reperfusion injury and an

N-BENZYLANILINE DERIVATIVE AND USES THEREOF

A N-benzylaniline derivative and uses thereof. The derivative is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound protects against cerebral ischemia/reperfusion injury and has analgesic action for chronic pat

Urea thiadiazole inhibitors of plasminogen activator inhibior-1

Methods of treating disorders associated with elevated levels of PAI-1 are disclosed comprising administering to a patient in need thereof a therapeutically effective amount of at least one compound of formula (I), or a pharmaceutically-acceptable salt, prodrug, stereoisomer or solvate thereof, wherein: A is aryl o heteroaryl, and R1-R12, are defined herein. The invention also pertains to pharmaceutical compositions and compounds within the scope of formula (I) as well as medicaments and articles of manufacture comprising compounds of formula (I).

Design and synthesis of highly potent and selective (2-arylcarbamoyl- phenoxy)-acetic acid inhibitors of aldose reductase for treatment of chronic diabetic complications

Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective (2-arylcarbamoyl-phenoxy)-acetic acid aldose reductase inhibitors. The compound class features a core template that utilizes an intramolecular hydrogen bond to position the key structural elements of the pharmacophore in a conformation, which promotes a high binding affinity. The lead candidate, example 40, 5-fluoro-2-(4-bromo-2-fluoro-benzylthiocarbamoyl)-phenoxyacetic acid, inhibits aldose reductase with an IC50 of 30 nM, while being 1100 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes. In addition, example 40 lowers nerve sorbitol levels with an ED50 of 31 mg/kg/d po in the 4-day STZ-induced diabetic rat model.

Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: Importance of additional hydrophobic aromatic interactions

Potent inhibitors of EGF-dependent protein tyrosine kinase (PTK) activity were synthesized in a series of 5-[(2,5-dihydroxybenzyl)amino]salicylates. Several of these compounds inhibited EGF-dependent DNA synthesis in ER 22 cells with IC50 1 μ

Oxalic acid ester derivatives

Disclosure herein is novel oxalic acid ester derivatives represented by the general formula: STR1 wherein either one of X and Y represents a nitro group, and the other represents STR2 in which R represents a lower alkyl group, and n represents a figure of