Category: 763114-26-7

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4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl] -2H-phthalazin-1-one: A novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1

Poly(ADP-ribose) polymerase activation is an immediate cellular response to metabolic-, chemical-, or ionizing radiation-induced DNA damage and represents a new target for cancer therapy. In this article, we disclose a novel series of substituted 4-benzyl-2H-phthalazin-1-ones that possess high inhibitory enzyme and cellular potency for both PARP-1 and PARP-2. Optimized compounds from the series also demonstrate good pharmacokinetic profiles, oral bioavailability, and activity in vivo in an SW620 colorectal cancer xenograft model. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl] -2H-phthalazin-1-one (KU-0059436, AZD2281) 47 is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Compound 47 is currently undergoing clinical development for the treatment of BRCA1- and BRCA2-defective cancers.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N793 – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. SDS of cas: 763114-26-7, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 763114-26-7, name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid. In an article£¬Which mentioned a new discovery about 763114-26-7

PHTHALAZINONE COMPOUND

4-(4-Fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one as crystalline Form C.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N744 – PubChem

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Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities

Poly (ADP-ribose) polymerase (PARP) inhibitors have achieved great success in clinical application, especially for the prolonged survival of cisplatin-sensitive ovarian cancer patients. However, there are still many patients who do not respond to PARP inhibitors. Novel PARP inhibitors with higher activity are urgently needed. Herein we report a series of compounds by molecular hybridization PARP-1 inhibitor Olaparib (Ola) with HSP90 inhibitor C0817 (one curcumin derivative). All synthesized compounds were evaluated for their antiproliferative activity in vitro, and some were further assessed for their inhibitory activities of the PARP enzyme and HSP90 affinity. Our results indicated that compound 4 could bind to HSP90 and cause static quenching, indicating that compound 4 was able to bind to HSP90, moreover, downstream molecular breast cancer 1 (BRAC-1) was reduced. In conclusion, dual target inhibitors of PARP and HSP90 exhibited stronger selective cytotoxicities against cancer.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N785 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Safety of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, 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

Olaparib-Based Photoaffinity Probes for PARP-1 Detection in Living Cells

The poly-ADP-ribose polymerase (PARP) is a protein from the family of ADP-ribosyltransferases that catalyzes polyadenosine diphosphate ribose (ADPR) formation in order to attract the DNA repair machinery to sites of DNA damage. The inhibition of PARP activity by olaparib can cause cell death, which is of clinical relevance in some tumor types. This demonstrates that quantification of PARP activity in the context of living cells is of great importance. In this work, we present the design, synthesis and biological evaluation of photo-activatable affinity probes inspired by the olaparib molecule that are equipped with a diazirine for covalent attachment upon activation by UV light and a ligation handle for the addition of a reporter group of choice. SDS-PAGE, western blotting and label-free LC-MS/MS quantification analysis show that the probes target the PARP-1 protein and are selectively outcompeted by olaparib; this suggests that they bind in the same enzymatic pocket. Proteomics data are available via ProteomeXchange with identifier PXD018661.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N784 – PubChem

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PIPERAZINOTRIZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF IN DRUG PREPARATION

Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.

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. Synthetic Route of 763114-26-7

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N779 – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. SDS of cas: 763114-26-7, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 763114-26-7, name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid. In an article£¬Which mentioned a new discovery about 763114-26-7

Synthesis and evaluation of a radioiodinated tracer with specificity for poly(ADP-ribose) polymerase-1 (PARP-1) in vivo

Interest in nuclear imaging of poly(ADP-ribose) polymerase-1 (PARP-1) has grown in recent years due to the ability of PARP-1 to act as a biomarker for glioblastoma and increased clinical use of PARP-1 inhibitors. This study reports the identification of a lead iodinated analog 5 of the clinical PARP-1 inhibitor olaparib as a potential single-photon emission computed tomography (SPECT) imaging agent. Compound 5 was shown to be a potent PARP-1 inhibitor in cell-free and cellular assays, and it exhibited mouse plasma stability but approximately 3-fold greater intrinsic clearance when compared to olaparib. An 123I-labeled version of 5 was generated using solid state halogen exchange methodology. Ex vivo biodistribution studies of [123I]5 in mice bearing subcutaneous glioblastoma xenografts revealed that the tracer had the ability to be retained in tumor tissue and bind to PARP-1 with specificity. These findings support further investigations of [123I]5 as a noninvasive PARP-1 SPECT imaging agent.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N802 – PubChem

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ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 763114-26-7

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N758 – PubChem

Application of 763114-26-7, 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. 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 kind of Phthalazinone derivatives and its use (by machine translation)

The present invention provides novel phthalazinone compounds and isomer thereof, pharmaceutically acceptable salts, solvates, chemically protected forms, and prodrugs; which can be used as PARP inhibitor and pharmaceutical compositions containing the novel phthalazinone compounds; wherein A, R1 and X are defined as shown. The medicine is used for the treatment of: vascular diseases, neurotoxicity, or diseases improved through the inhibition of PARP activity; or used as adjuvants for the treatment of cancers, or used for enhancing the therapeutic effect of radiation or chemotherapeutic agents on tumor cells, wherein the cancers includes breast cancer, ovarian cancer, colon cancer, melanoma, lung cancer, gastrointestinal stromal tumor, brain cancer, cervical cancer, pancreatic cancer, prostate cancer, gastric cancer, chronic myeloid leukocytes hypercytosis, liver canser, lymphoma, peritoneal cancer, soft tissue sarcoma, neuroendocrine tumors, advanced solid tumors, and glioblastoma.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 763114-26-7. In my other articles, you can also check out more blogs about 763114-26-7

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N769 – PubChem

Synthetic Route of 763114-26-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid,introducing its new discovery.

Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy

Concomitant inhibition of PARP and PI3K pathways has been recognized as a promising strategy for cancer therapy, which may expand the clinical utility of PARP inhibitors. Herein, we report the discovery of dual PARP/PI3K inhibitors that merge the pharmacophores of PARP and PI3K inhibitors. Among them, compound 15 stands out as the most promising candidate with potent inhibitory activities against both PARP-1/2 and PI3Kalpha/deltawith pIC50 values greater than 8. Compound 15 displayed superior antiproliferative profiles against both BRCA-deficient and BRCA-proficient cancer cells in cellular assays. The prominent synergistic effects produced by the concomitant inhibition of the two targets were elucidated by comprehensive biochemical and cellular mechanistic studies. In vivo, 15 showed more efficacious antitumor activity than the corresponding drug combination (Olaparib + BKM120) in the MDA-MB-468 xenograft model with a tumor growth inhibitory rate of 73.4% without causing observable toxic effects. All of the results indicate that 15, a first potent dual PARP/PI3K inhibitor, is a highly effective anticancer compound.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 763114-26-7, and how the biochemistry of the body works.Synthetic Route of 763114-26-7

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N786 – PubChem

763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, belongs to phthalazine compound, is a common compound. Quality Control of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acidIn an article, once mentioned the new application about 763114-26-7.

Benzene and [4, 5] imidazo [1, 2 – a] pyrazine ketone derivative and its preparation and use (by machine translation)

The invention provides a benzene and [4, 5] imidazo [1, 2 – a] pyrazine ketone derivatives and their pharmaceutically acceptable salt, its structure is shown as formula I. The invention also discloses containing benzo [4, 5] imidazo [1, 2 – a] pyrazine ketone derivatives preparation method and its in the preparation of antineoplastic drug in the preparation and application of PARP inhibitors. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N774 – PubChem