Discovery of 6-Bromocinnoline

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A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors

The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region and then building into the LPF shelf. Herein, we report the “hybridization” of a variety of KAc-binding fragments with a tetrahydroquinoline scaffold that makes optimal interactions with the LPF shelf, imparting enhanced potency and selectivity to the hybridized ligand. To demonstrate the utility of our hybridization approach, two analogues containing unique Asn binders and the optimized tetrahydroquinoline moiety were rapidly optimized to yield single-digit nanomolar inhibitors of CBP with exquisite selectivity over BRD4(1) and the broader bromodomain family.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 78593-33-6, molcular formula is C8H5BrN2, introducing its new discovery. 78593-33-6

Alkyl- or aryl-aminoalkoxy-benzene-sulfonyl indoles

The present invention relates to aminoalkoxyphenyl derivatives of formula: STR1 and its N-oxide and pharmaceutically acceptable salts, in which: B represents a–S–, –SO– or –SO2 — group, R1 and R2, which are identical or different, each denote hydrogen, a methyl or ethyl radial or a halogen atom, A denotes a straight-or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radial in which the hydroxy is optionally substituted by a lower alkyl radical, R3 denotes an alkkyl radical or a radical of formula: in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and Ar denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl group or lower alkoxy groups, R11 denotes hydrogen or a lower alkyl, phenyl, diphenylmethyl, benzyl or halogenobenzyl radical, R4 denotes hydrogen or an alkyl radical, or R3 and R4 when taken together denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by STR2 R represent hydrogen, an alkyl radical, a cycloalkyl radical, a benzyl radical or a phenyl radical optionally substituted with one or more substituents, which may be identical or different, selected from halogen atoms and from lower alkyl, lower alkoxy or nitro groups, are described. The compounds of the invention possess exceptional pharmacological properties, especially calcium transport inhibitory properties, as well as bradycardic, hypotensive and antiadrenergic properties.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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1-PROPANOL AND 1-PROPYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANDS

Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.875-66-1, Name is Cinnolin-4-ol, molecular formula is C8H6N2O, 875-66-1. In a Article, authors is Stanczak£¬once mentioned of 875-66-1

Synthesis and action on the central nervous system of some N2-substituted cinnoline derivatives

Alkylation of 4-hydroxycinnolines using ethyl bromoacetate resulted in N2-substituted acetic acids. These acids were converted to esters and amides. Some of the obtained acids were reduced with zinc dust to give 4-oxo-1,2,3,4-tetrahydro-2-cinnolineacetic acids. Several of the compounds were tested for their effect on central nervous system.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.875-66-1, Name is Cinnolin-4-ol, molecular formula is C8H6N2O, 875-66-1. In a Article, authors is Stanczak£¬once mentioned of 875-66-1

Synthesis, structures and biological activity of some 4-amino-3-cinnoline-carboxylic acid derivatives. Part 2

6,7,8-Substituted 4-amino-3-cinnolinecarboxylic acids 1 were condensed with amines to the corresponding 4-amino-3-cinnolinecarboxamides 7, 8. A variety of pharmacological tests showed a significant CNS activity of some new amides. Decarboxylation of 4-amino-3-cinnolinecarboxylic acids 1 yielded the corresponding 4-aminocinnolines 4 and alkaline hydrolysis of 1 gave 4-oxo-3-cinnolinecarboxylic acids 2. The acids 1 were converted into pyrimido[5,4-c]cinnolines 6 on two ways of synthesis.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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N-(unsubstituted or substituted)-4-substituted-6-(unsubstituted or substituted)phenoxy-2-pyridinecarboxamides or thiocarboxamides, processes for producing the same, and herbicides

N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I) and a process for producing the compound. A herbicide containing as an effective ingredient N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I).

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

Brief introduction of Cinnolin-4-ol

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Novel 4-(1H-1,2,3-triazol-4-yl)methoxy)cinnolines as potent antibacterial agents: Synthesis and molecular docking study

A new series of cinnoline-1,2,3-triazole derivatives were designed and synthesized by adopting Cu(1) catalyzed regeoselective1,3-dipolar cycloaddition reaction of terminal alkyne and azide. The in vitro antibacterial activity of all these compounds revealed that compounds 9d, 10a, 10b, and 10c are more potent antibacterial agents. Among the series, compound 4-(3-(4-((cinnolin-4-yloxy)methyl)-1H-1,2,3-triazol-1-yl)propyl)morpholine (10b) exhibited the most potent antibacterial activity against all tested gram-positive and gram-negative bacterial strains. Furthermore, molecular docking studies were also performed to understand the binding interactions of the most active analogs 9d, 10a, 10b, and 10c with Elastase of Pseudomonas aeruginosa (PDB: 1U4G). The results indicated that these classes of compounds have potential antibacterial activity, especially the compound 10b may serve as a promising antibacterial lead compound that could be further optimized for the further development of antibacterial drugs.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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78593-33-6, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 78593-33-6, name is 3-Bromocinnoline, introducing its new discovery.

ORGANIC LIGHT-EMITTING DEVICE, APPARATUS INCLUDING THE SAME, AND ORGANOMETALLIC COMPOUND

Provided are an organic light-emitting device, an apparatus including the organic light-emitting device, and an organometallic compound represented by Formula 1. The organic light-emitting device includes: a first electrode; a second electrode; and an organic layer between the first electrode and the second electrode and including an emission layer, wherein: the organic layer includes the organometallic compound represented by Formula 1.

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Cinnoline – Wikipedia,
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78593-33-6, Name is 3-Bromocinnoline, belongs to cinnoline compound, is a common compound. 78593-33-6In an article, authors is Ames, D. E., once mentioned the new application about 78593-33-6.

SOME REACTIONS OF 3-HALOGENOCINNOLINES CATALYSED BY PALLADIUM COMPOUNDS

3-Bromo-or 3-iodo-cinnoline (and 4-substituted analogues ) are condensed with terminal alkynes in the presence of Pd and Cu compounds as catalysts to give the 3-alkynyl-derivatives.When 4-chloro- or 4-phenoxy-compounds are used, the products react with amines, in the presence of copper(I) iodide, to form pyrrolo<3,2-c>cinnolines and with hydrazines to give either the same ring system or a pyrazolo<4,3-c>cinnoline.Hydrolysis of 3-alkynyl-4phenoxycinnoline to 3-alkynyl-4(1H)-cinnolinone, followed by cyclisation, yields the furo<3,2-c>cinnoline.Attempts to condense 3-halogenocinnolines with alkenes gave variable results: 3-phenyl ethenyl- and 3(2-pyridylethenyl)-4-(1H)-cinnolinones were obtained but 3-bromocinnoline gave the 3,3′-bicinnolinyl.Action of palladium acetate in the presence of ethyl acrylate converted 3-bromo-4-phenoxycinnoline into benzofuro<3,2-c>cinnoline and 3-bromo-4-phenylaminocinnoline into indolo<3,2-c>cinnoline.

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4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity

4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-beta-d-ribose 2?-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ?100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 < 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb. Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. 875-66-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 875-66-1, in my other articles.

Reference£º
Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics