Month: February 2021

253-52-1, Name is Phthalazine, belongs to phthalazine compound, is a common compound. Recommanded Product: PhthalazineIn an article, once mentioned the new application about 253-52-1.

Novel triazolophthalazine-hydrazone hybrids as potential PCAF inhibitors: Design, synthesis, in vitro anticancer evaluation, apoptosis, and molecular docking studies

Three novel series of triazolophthalazine derivatives bearing hydrazone moiety were designed, synthesized, and evaluated for their anticancer activity against four human cancer cell lines by MTT assay. Six derivatives demonstrated comparable activity with Doxorubicin reference drug against the selected cancer cells. Especially, compound 16 showed the most potent activity with IC50 values of 5.70, 8.04, 11.15, and 4.25, muM against HePG2, MCF-7, PC3, and HCT-116 respectively. Also, compound 26 exhibited comparable inhibitory effect with that of Doxorubicin against the selected cancer cell lines with IC50 values of 6.45, 8.63, 12.28, and 7.03 muM against HePG2, MCF-7, PC3, and HCT-116 respectively. Investigation of the apoptotic activity of the two most active compounds revealed that compounds 16 and 26 could induce both the early and the late apoptosis of HePG2. Further mechanistic study of the HePG2 cell cycle confirmed the spectacular cytotoxic and apoptotic effects of both compounds. Compounds 16 and 26 showed a pronounced increase in cells in G2/M and Pre G1 phases with a concomitant reduction of cells in G0-G1 and S phases. A follow up enzymatic assay indicated that these two compounds have comparable activities with that of bromosporine as PCAF inhibitors with IC50 values of 8.13 and 5.31 muM respectively. Moreover, molecular docking study for all the synthesized compounds was performed to predict their binding affinities toward the active site of histone acetyltransferase GCN5. Results of molecular docking were strongly correlated with that of the cytotoxicity study.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N18 – PubChem

Synthetic Route of 253-52-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 253-52-1, Name is Phthalazine,introducing its new discovery.

FACILE RADICAL DECARBOXYLATIVE ALKYLATION OF HETEROAROMATIC BASES USING CARBOXYLIC ACIDS AND TRIVALENT IODINE COMPOUNDS

Many kinds of heteroaromatic bases were easily alkylated by the reaction of carboxylic acids with benzene or pentafluorobenzene via radical decarboxylative pathways.This system was further applied to the reaction with tetrahydrofurylcarboxylic acid, 1-(2,3,5-tri-O-benzyl)-D-ribofuranosylacetic acid, and 1-(2,3,5-tri-O-benzyl)-D-ribofuranosylcarboxylic acid for the model synthesis of C-nucleosides.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N449 – PubChem

Reference of 763111-47-3, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2. In a Patent£¬once mentioned of 763111-47-3

A phthalazinone hydroxamic acid derivatives and its preparation method and application (by machine translation)

The invention discloses a has a plurality of poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) inhibitory activity of taitai qin alkone different hydroxy wo acid compounds and preparation method and application thereof. The taitai qin alkone different hydroxy wo acid compounds of the formula I as shown in the structural formula, wherein R1 Is a hydrogen atom or a halogen; R2 Is a hydrogen atom or a halogen; Y is an oxygen atom, methylene or fluorine substituted methylene; Z is or G bond is a chemical bond, methylene, fluoro methylene or double bond. In vitro cell proliferation experiment shows that, as shown in formula I compound well inhibit a variety of tumor cell proliferation. Poly adenosine diphosphate ribose polymerase (PARP) and histone deacetylase (HDAC) inhibition experiment I indicates the type compound is shown to poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) have good inhibitory activity of the compound. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N805 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: phthalazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, molecular formula is C16H11FN2O3

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

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

Electric Literature of 253-52-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 253-52-1, Name is Phthalazine,introducing its new discovery.

Evaluation of new dihydrophthalazine-appended 2,4-diaminopyrimidines against Bacillus anthracis: Improved syntheses using a new pincer complex

The synthesis and evaluation of ten new dihydrophthalazine-appended 2,4-diaminopyrimidines as potential drugs to treat Bacillus anthracis is reported. An improved synthesis utilizing a new pincer catalyst, dichlorobis[1-(dicyclohexylphosphanyl)-piperidine]palladium(II), allows the final Heck coupling to be performed at 90C using triethylamine as the base. These milder conditions have been used to achieve improved yields for new and previously reported substrates with functional groups that degrade or react at the normal 140C reaction temperature. An analytical protocol for separating the S and R enantiomers of two of the most active compounds is also disclosed. Finally, the X-ray structure for the most active enantiomer of the lead compound, (S)-RAB1, is given.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N304 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of Phthalazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 253-52-1, Name is Phthalazine, molecular formula is C8H6N2

Reaction of six-membered azaaromatics with allyltributyltin

Pyridazines were reacted with allyltributyltin in the presence of chloroformate to give 1-alkoxycarbonyl-6-allyl and 1-alkoxycarbonyl-4-allyldihydropyridazines as major and minor products, respectively. The reaction system was applied to other diazines and pyrimidine and pyrazine were shown to afford diallyltetrahydroadducts. Benzodiazines also gave allylation products in good yields. The reaction seems to be applicable to most six-membered azaaromatics.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N206 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: Phthalazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 253-52-1, Name is Phthalazine, molecular formula is C8H6N2

Sonogashira Reaction: Synthesis of Novel Derivatives of 3-Aryl-Substituted 6-Chloroimidazo[2, 1-a]phthalazines Catalyzed by Pd-Cu in Water

The reaction of 1-chloro-4-propargylaminophthalazine with various aryl halides catalyzed by Pd?Cu in the presence of potassium carbonate, as the base, in water leads to the one-pot formation of new derivatives of 3-aryl-substituted-6-chloroimidazo-[2, 1-a]phthalazines in moderate-to-good yields. Their structures are confirmed by IR and NMR spectra as well as elemental analyses. All the compounds prepared are screened in vitro for their anti-bacterial activities. The preliminary results indicate that some target compounds exhibit promising anti-bacterial potency.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N51 – PubChem

Synthetic Route of 763114-26-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, molecular formula is C16H11FN2O3. In a Patent£¬once mentioned of 763114-26-7

A method for preparing high-purity aurar handkerchief Nepal (by machine translation)

The invention discloses a method for preparing high-purity aurar handkerchief Nepal, is a 2-fluoro-5 – [(4-oxo -3,4-dihydrodi nitrogen phenodiazine-1-yl) methyl] benzoic acid as the starting material, is activated, aminolysis to obtain high-purity aurar handkerchief Nepal after crystallization, wherein the activation is to contain 2-fluoro-5 – [(4-oxo -3,4-dihydrodi nitrogen phenodiazine-1-yl) methyl] benzoic acid is added to a solution of carbonyl diimidazole activator, active amide intermediates made; without separation and purification of active amide intermediate, direct and 1-cyclopropanecarboxylic formyl piperazine aminolysis crystallization, aurar handkerchief Nepal prepared. The method of the invention the purity of the aurar handkerchief Nepal preparation of greater than 99.8%, the craft is simple, high yield, low cost, is more suitable for industrial production. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N776 – PubChem

Synthetic Route of 253-52-1, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 253-52-1, Name is Phthalazine, molecular formula is C8H6N2. In a Article£¬once mentioned of 253-52-1

PHTHALAZINE DERIVATIVES FROM AROMATIC ALDAZINES

A Lewis acid mediated synthesis of phthalazine derivatives II and III from aromatic aldazines I is reported.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N367 – PubChem