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Different fumarine derivative and its preparation method and application (by machine translation)

The invention discloses a different fumarine the chemical structure of the derivative (the formula ), Through the NICD amino with aryl isocyanate, carboxylic acid, amide carbonyl chloride condensation reaction or NICD with aromatic amino through solid phosgene symmetrical amide prepared by the condensation reaction, the compound has certain in vivo and in vitro anti-cancer activity, can be used as a cancer prevention and treatment of drug application. type Formula In the chemical structure: . (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N750 – PubChem

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PHTHALAZINONE KETONE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL USE THEREOF

A phthalazinone ketone derivative as represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the derivative, a use thereof as a poly (ADP-ribose) polymerase (PARP) inhibitor, and a cancer treatment method thereof are described.

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Compound based on ligand-CRBN induced degradation PARP-1 of ligand, as well as preparation method and application thereof (by machine translation)

The compound and the pharmaceutical composition of the CRBN compound disclosed PARP – 1 by the invention can be used for preventing, or treating a human PARP – 1 body, and E3 the compound and the cereblon pharmaceutical composition disclosed by the invention can. be used for preventing or treating a human body and having a great application prospect in, and the field of medicines / PARP – 1, PARP – 1, PARP – 1. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N778 – PubChem

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Simple preparation method 4 -substituted-methyl -1 – (2H) phthalazinone (by machine translation)

The invention relates to a simple preparation method. 4 -substituent methyl -1 – (2H) phthalazinone (I). The method utilizes diG substituted benzene (II) and a compound III compound in the presence of a solvent A and an alkali, and the compound, the compound of formula IV or the compound of formula IV and hydrazine hydrate are condensed to prepare 4 – (pyridin -4 – yl) methyl -1 – (2H) phthalazinone (IA) or 4 – (4 – fluoro -3 – carboxyphenyl) methyl -1 – (2H) phthalazinone (IB), respectively. The method can be used for preparing taditinib and ornisonil. The method is simple in technological process, high in reaction repeatability, easy to operate, good in product stability, and high in purity. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N759 – PubChem

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HETEROCYCLIC-IMIDAZOLE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention relates to a heterocyclic-imidazole derivative, a preparation method therefor, and a medical use thereof, and particularly to a new heterocyclic-imidazole derivative of general Formula (I), a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof as a therapeutic agent, particularly as a poly(ADP-ribose)polymerase (PARP) inhibitor.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N738 – 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,
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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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Phthalazine – Wikipedia,
Phthalazine | C8H6N789 – PubChem

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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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Phthalazine – Wikipedia,
Phthalazine | C8H6N776 – PubChem

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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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Phthalazine – Wikipedia,
Phthalazine | C8H6N798 – 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,
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