Archives for Chemistry Experiments of 763114-26-7

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 763114-26-7

Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 ¡À 1.25 nM) and MDA-MB-436 cancer cell (11.62 ¡À 2.15 muM), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer?s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 ¡À 0.91 muM) which was stronger than neostigmine (12.01 ¡À 0.45 muM) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer?s disease.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N789 – PubChem

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RADIOLABELLED COMPOUND

The present invention relates to radiolabelled olaparib and in particular [ 18 F]olaparib, a process for producing radiolabelled olaparib, and uses of radiolabelled olaparib in medical imaging.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N742 – PubChem

Discovery of 4-(4-Chlorobenzyl)phthalazin-1(2H)-one

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 53242-88-9, help many people in the next few years.COA of Formula: C15H11ClN2O

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PHENYL PHTHALAZINE DERIVATIVE, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to a compound represented by Chemical Formula 1, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of cardiovascular diseases.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N720 – PubChem

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Containing the phthalazine -1 (2 H) – one structure of PARP inhibitor, its manufacturing method and medical use (by machine translation)

The invention relates to the field of pharmaceutical chemistry, and in particular relates to a class of 4 – (4 – fluoro – 3 – (1, 2, 3, 4 – tetrahydrobenz [4, 5] imidazo [1, 2 – a] pyrazine – 2 – carbonyl) benzyl) phthalazine – 1 (2 H) – ketone derivative (I), wherein R are defined in the specification, the invention also discloses a process for their preparation, and pharmaceutical compositions containing these compounds, the pharmacodynamics tests prove that, the compounds of this invention have PARP inhibitory activity, can be used as single therapeutic agents tumor, or in combination with other anti-tumor drugs, thereby improving the existing anti-tumor drug effectiveness and reduced dose and toxicity of role. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N782 – PubChem

A new application about 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 763114-26-7 is helpful to your research. Related Products of 763114-26-7

Related Products of 763114-26-7, 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, 763114-26-7, molcular formula is C16H11FN2O3, introducing its new discovery.

Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase

We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold. Subsequent optimisation of inhibitory activity, metabolic stability and pharmacokinetic parameters has led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-one PARP-1 inhibitors which retain low nM cellular activity and show good stability in vivo and efficacy in cell based models.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N787 – PubChem

The Absolute Best Science Experiment for 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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Design, synthesis, and anticancer properties of isocorydine derivatives

Isocorydine (ICD), an aporphine alkaloid, is widely distributed in nature. Its ability to target side population (SP) cells found in human hepatocellular carcinoma (HCC) makes it and its derivative 8-amino-isocorydine (NICD) promising chemotherapeutic agents for the treatment of HCC. To improve the anticancer activity of isocorydine derivatives, twenty derivatives of NICD were designed and synthesized through chemical structure modifications of the aromatic amino group at C-8. The anti-proliferative activities of all synthesized compounds against human hepatocellular (HepG2), cervical (HeLa), and gastric (MGC-803) cancer cell lines were evaluated using an MTT assay. The results showed that all the synthetic compounds had some tumor cell growth inhibitory activity. The compound COM33 (24) was the most active with IC50 values under 10 muM (IC50 for HepG2 = 7.51 muM; IC50 for HeLa = 6.32 muM). FICD (12) and COM33 (24) were selected for further investigation of their in vitro and in vivo activities due to their relatively good antiproliferative properties. These two compounds significantly downregulated the expression of four key proteins (C-Myc, beta-Catenin, CylinD1, and Ki67) in HepG2 cells. The tumor inhibition rate of COM33 (24) in vivo was 73.8% after a dose 100 mg/kg via intraperitoneal injection and the combined inhibition rate of COM33 (24) (50 mg/kg) with sorafenib (50 mg/kg) was 66.5%. The results indicated that these isocorydine derivatives could potentially be used as targeted chemotherapy agents or could be further developed in combination with conventional chemotherapy drugs to target cancer stem cells (CSCs) and epithelial-to-mesenchymal transition (EMT), the main therapeutic targets in HCC.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N798 – PubChem

Final Thoughts on Chemistry for 4-Bromophthalazin-1(2H)-one

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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, 19064-73-4, name is 4-Bromophthalazin-1(2H)-one, introducing its new discovery. Recommanded Product: 4-Bromophthalazin-1(2H)-one

Synthesis and biological evaluation of 2,4-disubstituted phthalazinones as Aurora kinase inhibitors

A series of 2,4-disubstituted phthalazinones were synthesized and their biological activities, including antiproliferation, inhibition against Aurora kinases and cell cycle effects were evaluated. Among them, N-cyclohexyl-4-((4-(1-methyl-1H-pyrazol-4-yl)-1-oxophthalazin-2(1H)-yl) methyl) benzamide (12c) exhibited the most potent antiproliferation against five carcinoma cell lines (HeLa, A549, HepG2, LoVo and HCT116 cells) with IC50 values in range of 2.2?4.6 muM, while the IC50 value of reference compound VX-680 was 8.5?15.3 muM. Moreover, Aurora kinase assays exhibited that compound 12c was potent inhibitor of AurA and AurB kinase with the IC50 values were 118 ¡À 8.1 and 80 ¡À 4.2 nM, respectively. Molecular docking studies indicated that compound 12c forms better interaction with both AurA and AurB. Furthermore, compound 12c induced G2/M cell cycle arrest in HeLa cells by regulating protein levels of cyclinB1 and cdc2. These results suggested that 12c is a promising pan-Aurora kinase inhibitor for the potential treatment of cancer.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N701 – PubChem

Extended knowledge of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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A heterocyclic and imidazole compound, its pharmaceutical composition and its preparation and use (by machine translation)

The invention relates to a heterocyclic and imidazole derivatives, their preparation and their use in medicine. In particular, the invention relates to a compound of general formula (I) indicated by the new heterocyclic and imidazole derivatives, preparation method thereof and a pharmaceutical composition containing the derivative and its as therapeutic agents in particular as poly (ADP – ribose) polymerase (PARP) inhibitors. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N736 – PubChem

More research is needed about 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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PHTHALAZINONE DERIVATIVE

4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N753 – PubChem

Archives for Chemistry Experiments of 7-Bromophthalazin-1(2H)-one

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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinical development for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia-ventricular fibrillation (VT-VF). We will describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improved from the first generation late INa inhibitor 1 (ranolazine). Compound 4 was 42 times more potent than 1 in reducing ischemic burden in vivo (S-T segment elevation, 15 min left anteriorior descending, LAD, occlusion in rabbits) with EC50 values of 190 and 8000 nM, respectively. Compound 4 represents a new class of potent late INa inhibitors that will be useful in delineating the role of inhibitors of this current in the treatment of patients.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N713 – PubChem