Category: 763111-47-3

Synthetic Route 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 Article£¬once mentioned of 763111-47-3

Effect of small-molecule modification on single-cell pharmacokinetics of PARP inhibitors

The heterogeneous delivery of drugs in tumors is an established process contributing to variability in treatment outcome. Despite the general acceptance of variable delivery, the study of the underlying causes is challenging, given the complex tumor microenvironment including intra- and intertumor heterogeneity. The difficulty in studying this distribution is even more significant for small-molecule drugs where radiolabeled compounds or mass spectrometry detection lack the spatial and temporal resolution required to quantify the kinetics of drug distribution in vivo. In this work, we take advantage of the synthesis of fluorescent drug conjugates that retain their target binding but are designed with different physiochemical and thus pharmacokinetic properties. Using these probes,wefollowed the drug distribution in cell culture and tumor xenografts with temporal resolution of seconds and subcellular spatial resolution. These measurements, including in vivo permeability of small-molecule drugs, can be used directly in predictive pharmacokinetic models for the design of therapeutics and companion imaging agents as demonstrated by a finite element model. Mol Cancer Ther; 13(4); 986-95.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N829 – PubChem

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A process for preparing 1 – [5 – [(3, 4 – dihydro -4 – oxo -1 – taitai qin base) methyl] -2 – fluoro benzoyl] piperazine (by machine translation)

The present invention provides a process for preparing 1 – [5 – [(3, 4 – dihydro -4 – oxo -1 – taitai qin base) methyl] -2 – fluoro benzoyl] piperazine (compound of formula I) of the method, including: 1 – [5 – [(3, 4 – dihydro -4 – oxo -1 – taitai qin base) methyl] -2 – fluoro benzoic acid piperazine and piperazine proton acid salt in a solvent to react under the acid condition 0.1 – 36 hours, and then adding a base salt free, to obtain the product. Preparation method of the invention, the process is simple, can be large-scale production, the price of the material is low, production cost can be reduced, and higher yield. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N803 – PubChem

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PROCESS FOR THE PREPARATION OF OLAPARIB AND POLYMORPHS THEREOF

The present invention is directed to process for preparation of Olaparib of formula (I). The present invention further relates to novel polymorphic forms of Olaparib, pharmaceutical compositions containing them, and method of treatment using the same.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N813 – PubChem

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Controlling cellular distribution of drugs with permeability modifying moieties

Phenotypic screening provides compounds with very limited target cellular localization data. In order to select the most appropriate target identification methods, determining if a compound acts at the cell-surface or intracellularly can be very valuable. In addition, controlling cell-permeability of targeted therapeutics such as antibody-drug conjugates (ADCs) and targeted nanoparticle formulations can reduce toxicity from extracellular release of drug in undesired tissues or direct activity in bystander cells. By incorporating highly polar, anionic moieties via short polyethylene glycol linkers into compounds with known intracellular, and cell-surface targets, we have been able to correlate the cellular activity of compounds with their subcellular site of action. For compounds with nuclear (Brd, PARP) or cytosolic (dasatinib, NAMPT) targets, addition of the permeability modifying group (small sulfonic acid, polycarboxylic acid, or a polysulfonated fluorescent dye) results in near complete loss of biological activity in cell-based assays. For cell-surface targets (H3, 5HT1A, beta2AR) significant activity was maintained for all conjugates, but the results were more nuanced in that the modifiers impacted binding/activity of the resulting conjugates. Taken together, these results demonstrate that small anionic compounds can be used to control cell-permeability independent of on-target activity and should find utility in guiding target deconvolution studies and controlling drug distribution of targeted therapeutics.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N827 – PubChem

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A one-pot radioiodination of aryl amines: Via stable diazonium salts: Preparation of 125I-imaging agents

An operationally simple, one-pot, two-step tandem procedure that allows the incorporation of radioactive iodine into aryl amines via stable diazonium salts is described. The mild conditions are tolerant of various functional groups and substitution patterns, allowing late-stage, rapid access to a wide range of 125I-labelled aryl compounds and SPECT radiotracers.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N828 – PubChem

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SUBSTITUTED 4-(4-FLUORO-3-(PIPERAZINE-1- CARBONYL)BENZYL)PHTHALAZIN-1(2H)-ONE DERIVATIVES AS POLY (ADP-RIBOSE) POLYMERASE-1 INHIBITORS

Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly (ADP-ribose) polymerase- 1 inhibitors (PARP-1 inhibitors).

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Phthalazine – Wikipedia,
Phthalazine | C8H6N812 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Computed Properties of C20H19FN4O2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2

PHTHALAZINONE DERIVATIVES

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Phthalazine – Wikipedia,
Phthalazine | C8H6N809 – PubChem

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PHTHALAZINONE DERIVATIVES

This review tries to shed light on the early history of different methods for the generation of N-heterocyclic carbenes (NHCs), i.e., the extrusion of heterocumulenes (decarboxylations) from suitable mesomeric betaines, deprotonations of hetarenium salts, alpha-eliminations, tautomerizations of mesomeric betaines, and reductive desulfurizations of cyclic thioureas. Selected examples of acyclic and three- to eight-membered NHCs are presented, as well the generation of selected five- and six-membered anionic NHCs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N814 – PubChem

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, 763111-47-3, name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, introducing its new discovery. COA of Formula: C20H19FN4O2

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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Phthalazine – Wikipedia,
Phthalazine | C8H6N804 – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 763111-47-3, name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one. In an article£¬Which mentioned a new discovery about 763111-47-3

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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Phthalazine – Wikipedia,
Phthalazine | C8H6N818 – PubChem