Category: 763114-26-7

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, 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

Identification and preclinical characterization of a novel and potent poly?(ADP-ribose) polymerase (PARP) inhibitor ZYTP1

Purpose: Poly(ADP-ribose) polymerase-1 (PARP-1) is a nuclear enzyme involved in the detection and repair of DNA damage. Studies have shown that inhibition of PARP and Tankyrase (TNKS) has significant antitumor effect in several types of cancers including BRCA-negative breast cancers. Methods: Identification of ZYTP1, a novel PARP inhibitor, through a battery of in vitro assays and in vivo studies. PARP and TNKS inhibitory activity of ZYTP1 was assessed in cell-free kinase assay. In vitro cell killing potency of ZYTP1 was tested in a panel of cell lines including BRCA-negative cells. ZYTP1 was also tested in xenograft models in combination with temozolomide (TMZ). The pharmacokinetic profile of ZYTP1 was determined in rodent and non-rodent preclinical species. Safety of ZYTP1 was assessed in Wistar rats and Beagle dogs upon repeated dosing. Results: ZYTP1 inhibited PARP1, PARP2, Tankyrase-1 and Tankyrase-2 with IC50 of 5.4, 0.7, 133.3 and 289.8?nM, respectively, and additionally trapped PARP1 onto damaged DNA. It also potentiated MMS-mediated killing of different cancer cell lines. Compound demonstrated good Caco-2 cell permeability. The oral bioavailability of ZYTP1 in mice, rats and dogs ranged between 40 and 79% and demonstrated efficacy in colon cancer xenograft model at a dose of 1?10?mg/kg in combination with TMZ. In a 28-day repeat dosing, oral toxicity study in rats, it was found to show > 10¡Á safety margin. Conclusions: ZYTP1 is a novel PARP inhibitor that showed potential for development as a treatment for various solid tumors.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N790 – PubChem

Application of 763114-26-7, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.763114-26-7, Name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, molecular formula is C16H11FN2O3. In a article£¬once mentioned of 763114-26-7

Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors

Currently, synergistic inhibition of poly(ADP-ribose) polymerase-1 (PARP-1) and histone deacetylases (HDACs) has been a potential effective strategy for cancer treatment. Herein, by combining critical pharmacophores in approved drugs olaparib and chidamide, a series of novel 2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid derivatives were designed and synthesized. All efforts led to a good dual PARP-1/HDAC-1 inhibitor, compound 4, with IC50 values of 4.2 and 340 nM against PARP-1 and HDAC-1, which were as potent as olaparib and chidamide respectively. The MTT assay further demonstrated that compound 4 had potent inhibitory activities against BRCA1/2-proficient K562 and MDA-MB-231 cells with GI50 values of 5.6 and 4.3 muM, respectively. Therefore, our results suggested that compound 4 could be a promising dual PARP-1/HDAC-1 inhibitor for further studies. In addition, a few excellent PARP-1 inhibitors such as 7?9 and HDAC-1 inhibitors such as 12 were serendipitously discovered, which also could be further studied in our next work.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N791 – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. HPLC of Formula: C16H11FN2O3, 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

PHTHALAZINONE DERIVATIVES

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Phthalazine – Wikipedia,
Phthalazine | C8H6N757 – PubChem

Related Products 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

SUBSTITUTED PHTHALAZIN-1 (2H)-ONE DERIVATIVES AS SELECTIVE INHIBITORS OF POLY (ADP-RIBOSE) POLYMERASE-1

The present invention relates to novel compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to a process of preparing novel compounds of general formula (I), their stereoisomers, regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis. The compounds of formula (I) are useful as PARP-1 inhibitors for the treatment of, e.g. cancer.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N764 – PubChem

Synthetic Route 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.

Design, synthesis and biological evaluation of novel phthalazinone acridine derivatives as dual PARP and Topo inhibitors for potential anticancer agents

In this study, we designed and synthesized a series of phthalazinone acridine derivatives as dual PARP and Topo inhibitors. MTT assays indicated that most of the compounds significantly inhibited multiple cancer cells proliferation. In addition, all the compounds displayed Topo II inhibition activity at 10 mol/L, and also possessed good PARP-1 inhibitory activities. Subsequent mechanistic studies showed that compound 9a induced remarkable apoptosis and caused prominent S cell cycle arrest in HCT116 cells. Our study suggested that 9a inhibiting Topo and PARP concurrently can be a potential lead compound for cancer therapy.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N788 – 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. Recommanded Product: 763114-26-7In an article, once mentioned the new application about 763114-26-7.

PHTHALAZINONE DERIVATIVES

A compound of the formula (I) wherein: A and B together represent an optionally substituted, fused aromatic ring, X is selected from H and F, R1 and R2 are independently selected from H and methyl, RN1 is selected from H and optionally substituted C1-7 alkyl, RN2 is selected from H, optionally substituted C1-7 alkyl, C3-7 heterocyclyl and C5-6 aryl, or RN1 and RN2 and the nitrogen atom to which they are bound form an optionally substituted nitrogen containing C5-7 heterocyclic group

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Phthalazine – Wikipedia,
Phthalazine | C8H6N755 – PubChem

Related Products 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 PARP inhibitor, its pharmaceutical composition, preparation method and application (by machine translation)

The invention provides a PARP inhibitor, its pharmaceutical composition, preparation method and application, which belongs to the field of medicine. The PARP inhibitor, its pharmaceutically acceptable salt, hydrate, solvate, metabolic precursor or prodrug of formula (I) is shown. The preparation method comprises: in an inert solvent, of formula (a) compound of the formula (b) compound in the presence of condensing agent and alkaline reagent under, the reaction is carried out, to obtain states the type (I) compounds. In addition also discloses a formula (I) indicated by the PARP inhibitor, its pharmaceutically acceptable salt, hydrate, solvate, metabolic precursor or prodrug in preparation for preventing or treating tumor application of the medicament. The present invention provides this kind of PARP inhibitor has excellent anti-PARP activity, can be used for preparing a plurality of anti-tumor pharmaceutical preparations (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N773 – PubChem

Electric Literature 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

Phthalazinone derivatives pro or its pharmaceutically acceptable salt and its pharmaceutical composition and application (by machine translation)

The invention belongs to the technical field of pharmaceutical chemistry, in particular to a phthalazinone derivative pro or its pharmaceutically acceptable salt, also relates to a pharmaceutical composition and in the preparation of an anti-tumor drug. The present invention provides compounds having the structural formula (I) Of the phthalazinone derivatives prodrugs of good solubility in vivo, after administration into the body, by the metabolic release phthalazine ketone drug molecules, thereby greatly improving the phthalazine ketone group in vivo bioavailability of drug molecules, the phthalazine ketone drug molecules with the in vivo enzyme PARP to not reversible way binding to exert the drug efficacy, anti-tumor activity is prominent. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N739 – PubChem

763114-26-7, Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 763114-26-7

Phthalazinone derivatives pro or its pharmaceutically acceptable salt and its pharmaceutical composition and application (by machine translation)

The invention belongs to the technical field of pharmaceutical chemistry, in particular to a phthalazinone derivative pro or its pharmaceutically acceptable salt, also relates to a pharmaceutical composition and in the preparation of an anti-tumor drug. The present invention provides compounds having the structural formula (I) Of the phthalazinone derivatives prodrugs of good solubility in vivo, after administration into the body, by the metabolic release phthalazine ketone drug molecules, thereby greatly improving the phthalazine ketone group in vivo bioavailability of drug molecules, the phthalazine ketone drug molecules with the in vivo enzyme PARP to not reversible way binding to exert the drug efficacy, anti-tumor activity is prominent. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N739 – PubChem

763114-26-7, 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, 763114-26-7, name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, introducing its new discovery.

HETEROCYCLIC DERIVATES, PREPARATION PROCESSES AND MEDICAL USES THEREOF

Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.763114-26-7, you can also check out more blogs about763114-26-7

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N741 – PubChem