388-31-8

Usage

InChI:InChI=1/C12H8BrFO/c13-7-12(15)10-5-6-11(14)9-4-2-1-3-8(9)10/h1-6H,7H2

Upstream product

• 316-68-7 4-fluoro-1-acetonaphthone 

Downstream Products

• 388-62-5 3-bromo-1-[2-(4-fluoro-[1]naphthyl)-2-oxo-ethyl]-pyridinium; bromide 
• 72326-42-2 1-(4-Fluoro-naphthalen-1-yl)-2-phenylamino-ethanone 

Relevant academic research and scientific papers

Novel Aryl-Substituted Pyrimidones as Inhibitors of 3-Mercaptopyruvate Sulfurtransferase with Antiproliferative Efficacy in Colon Cancer

The enzyme 3-mercaptopyruvate sulfurtransferase (3-MST) is one of the more recently identified mammalian sources of H2S. A recent study identified several novel 3-MST inhibitors with micromolar potency. Among those, (2-[(4-hydroxy-6-methylpyrimidin-2-yl)sulfanyl]-1-(naphthalen-1-yl)ethan-1-one) or HMPSNE was found to be the most potent and selective. We now took the central core of this compound and modified the pyrimidone and the arylketone sides independently. A 63-compound library was synthesized; compounds were tested for H2S generation from recombinant 3-MST in vitro. Active compounds were subsequently tested to elucidate their potency and selectivity. Computer modeling studies have delineated some of the key structural features necessary for binding to the 3-MST's active site. Six novel 3-MST inhibitors were tested in cell-based assays: they exerted inhibitory effects in murine MC38 and CT26 colon cancer cell proliferation; the antiproliferative effect of the compound with the highest potency and best cell-based activity (1b) was also confirmed on the growth of MC38 tumors in mice.

Heterocyclic Compound

The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention shows a strong IAP antagonistic activity.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including inflammatory and immune diseases, having the structure of formula (I): an en

DIHYDROIMIDAZOTHIAZOLE DERIVATIVES

Compounds of formula (I): or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.

HETEROCYCLIC MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of Formula (I) or stereoisomers or prodrugs or solvates or pharmaceutically acceptable salts thereof, wherein A, B, J, K, Z, R, Ra, Rb, Rc, and Rd, are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

Tricyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-kB activity and use thereof

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KB ACTIVITY AND USE THEREOF

Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF- KB activity including obesity, diabetes, inflammatory and immune diseases, and have the

Modulators of the glucocorticoid receptor, AP-1, and/or NF-kappaB activity and use thereof

A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have the

5-HT2B RECEPTOR ANTAGONISTS

Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.

Acid Catalysed Prototropy of Substituted Acetonaphthones - Kinetics of Perchloric Acid Catalysed Bromination and Phenyl Iodosoacetate Oxidation

Enolisation rates of several 4-substituted 1-acetonaphthones and 6-substituted 2-acetonaphthones at three different temperatures in acetic acid-water mixture (95percent, v/v) in perchloric acid catalysed bromination and phenyl iodosoacetate (PIA) oxidation reactions correlate very well with Hammett ?p constants.Acetonaphthones with 4- and 6-OCH3 substituents deviate from the corresponding Hammett plot for PIA oxidation.From basicity data deprotonation rate constants (kd) have been evaluated for bromination and PIA oxidation reactions.