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AKT PROTEIN KINASE INHIBITORS

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

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Cinnoline – Wikipedia,
Cinnoline – an overview | ScienceDirect Topics

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Solid-phase synthesis of substituted cinnolines by a Richter type cleavage protocol

Starting from triazene bound ortho-halo arenes on a solid support, palladium-catalyzed alkynylations and subsequent cleavage reactions under acidic conditions give rise to ortho-alkynylaryldiazonium salts, which in turn undergo cyclization to afford substituted 4-halo- and 4- hydroxycinnolines in moderate to good yields. The method is applicable to automated synthesis.

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Cinnoline – Wikipedia,
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Method for preparing 4-hydroxycinnolines in a pH controlled system

In the preparation of a 4-hydroxycinnoline wherein the diazonium salt of a 2-aminoacetophenone in aqueous solution is allowed to undergo cyclocondensation, the improvement that comprises maintaining the pH of the solution between about 4.0 and 8.5 during the cyclocondensation.

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Cinnoline – Wikipedia,
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Metallation of diazines XIV. First O-directed metallation of cinnolines. Metallation of 3-, 4-chloro and 3-, 4-methoxycinnolines

The lithiation of 3-, 4-chloro and 3-, 4-methoxycinnolines was studied and good yields were obtained. When iodine was used as electrophile, 4,8-diiodo or 4,8-iodochloro compounds were prepared. A xanthone and diazepine were synthetized.

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Cinnoline – Wikipedia,
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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,
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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,
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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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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,
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875-66-1, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 875-66-1, Name is Cinnolin-4-ol, molecular formula is C8H6N2O. In a Article, authors is Naik, Maruti£¬once mentioned of 875-66-1

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.

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Cinnoline – Wikipedia,
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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Gautheron Chapoulaud and a compound is mentioned, 875-66-1, Cinnolin-4-ol, introducing its new discovery. 875-66-1

Synthesis of 4,8-diarylcinnolines and quinazolines with potential applications in nonlinear optics. Diazines. Part 28

New 4,8-diarylbenzodiazines have been synthesized using cross-coupling reactions and regioselective metalation at the peri-position C8 of the benzene moiety of various cinnolines and quinazolines. Some of these compounds have been tested to assess their nonlinear optical properties. (C) 2000 Elsevier Science Ltd.

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