Day: March 9, 2021

Reference of 21725-69-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.21725-69-9, Name is Benzo[d]isoxazol-3-ol, molecular formula is C7H5NO2. In a Article£¬once mentioned of 21725-69-9

Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer

3-Phosphoglycerate dehydrogenase (PHGDH) has recently been identified as an attractive target in cancer therapy as it links upregulated glycolytic flux to increased biomass production in cancer cells. PHGDH catalyses the first step in the serine synthesis pathway and thus diverts glycolytic flux into serine synthesis. We have used siRNA-mediated suppression of PHGDH expression to show that PHGDH is a potential therapeutic target in PHGDH-amplified breast cancer. Knockdown caused reduced proliferation in the PHGDH-amplified cell line MDA-MB-468, whereas breast cancer cells with low PHGDH expression or with elevated PHGDH expression in the absence of genomic amplification were not affected. As a first step towards design of a chemical probe for PHGDH, we report a fragment-based drug discovery approach for the identification of PHGDH inhibitors. We designed a truncated PHGDH construct that gave crystals which diffracted to high resolution, and could be used for fragment soaking. 15 fragments stabilising PHGDH were identified using a thermal shift assay and validated by X-ray crystallography and ITC competition experiments to exhibit 1.5-26.2 mM affinity for PHGDH. A structure-guided fragment growing approach was applied to the PHGDH binders from the initial screen, yielding greater understanding of the binding site and suggesting routes to achieve higher affinity NAD-competitive inhibitors.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Electric Literature of 65685-55-4, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 65685-55-4, Name is Benzo[d]isoxazol-6-ol, molecular formula is C7H5NO2, introducing its new discovery.

Hypoxia-Selective Antitumor Agents. 3. Relationships between Structure and Cytotoxicity against Cultured Tumor Cells for Substituted N,N-Bis(2-chloroethyl)anilines

A series of aniline mustards with a wide range of electron-donating and -withdrawing substituents in the 3- and 4-positions has been synthesized and evaluated for cytotoxicity in cell culture to examine the potential of using nitro group deactivated nitrogen mustards for the design of novel hypoxia-selective anticancer drugs (Denny, W.A.; Wilson, W.R.J.Med Chem. 1986, 29, 879).Hydrolytic half-lives in tissue culture media, determined by bioassay against a cell line (UV4) defective in the repair of DNA interstrand cross-links showed the expected dependence on the Hammett electronic parameter, ?, varying from 0.13 h for the 4-amino analogue to >100 h for analogues with strongly electron-withdrawing substituents.Cytotoxic potencies in aerobic UV4 cultures showed a similar dependence on ?.This dependence predicted that the 4-nitroaniline mustard would be 7200-fold less potent than its potential six-electron reduction product, the 4-amino compound, in growth inhibition assays using a 1-h drug exposure.The measured differential was much lower (225-fold) because of the instability of the latter compound, but a differential of 17500-fold was observed in the initial rate of killing by using a clonogenic assay.The potential for formation of reactive mustards by reduction to the amine or hydroxylamine was demonstrated by the 4-nitroso compound, which had an aerobic toxicity similar to that of the amine.Although these features confirmed the original rationale, the 3-nitro- and 4-nitroaniline mustards had only minimal hypoxic selectivity against UV cells.Toxicity to hypoxic cells appears to be limited by the low reduction potentials of these compounds and consequent lack of enzymatic nitroreduction.However, this study has demonstrated that nitro groups can be used to latentiate aromatic nitrogen mustards and indicates that examples with higher reduction potentials could provide useful hypoxia-selective therapeutic agents.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Synthetic Route of 36216-80-5, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 36216-80-5, Benzo[d]isoxazol-3-amine, introducing its new discovery.

4-Amino-1,2,3-benzoxathiazine-Derivatives as Pesticides

The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

65685-55-4, Name is Benzo[d]isoxazol-6-ol, belongs to Benzisoxazole compound, is a common compound. name: Benzo[d]isoxazol-6-olIn an article, once mentioned the new research about 65685-55-4.

The Stereochemistry of 4,8-Dimethyl-6-phenyl-5,6,7,8-tetrahydro-4H-1,3,6-dioxazocin-2-ones Using NMR

Two isomeric 4,8-dimethyl-6-phenyl-5,6,7,8-tetrahydro-4H-1,3,6-dioxazocin-2-ones were prepared, and their pmr and cmr spectra were examined.From the tris(dipivaloylmethanato) europium (Eu(dpm)3) shift reagent and the dihedral angle, the title compounds are found to exist in the eq-ax and eq-eq methyl groups with boat-chair form.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 16263-52-8, Name is 3-Chloro-1,2-benzisoxazole,introducing its new discovery., SDS of cas: 16263-52-8

BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY

The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R 1) n represents 0, 1, or 2 substituents, which can be the same or different, from the group C 1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono-or dialkyl (C 1-2)-amino, sulfonyl-(C 1-3)alkyl or-alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono-or dialkyl (C 1-2)-amino, X is O, S, NH or NCH 3, Y represents CH 2, or (CH 2) 2, (R 2) m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R 2) mis a methylene bridge or ethylene bridge, A is a group–CH 2–(CRH) p–wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2-or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono-or dialkyl (C 1-2)amino, sulfonyl-(C 1-3)alkyl or-alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono-or dialkyl (C 1-2)-amino.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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 a patent, 21725-69-9, molecular formula is C7H5NO2, introducing its new discovery. SDS of cas: 21725-69-9

BENZISOXAZOLES

The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R1; Y is absent when X represents -Z-R1 and -(C=O)-R6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR 5-carbonyl-; R1 represents C1-4alkyl, Ar1, Ar1-C1-4a1ky1-, -NR3R4 or -Het1; R2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C1-4alkyloxy or C1-4alkyl; R3 and R4 are each independently selected from hydrogen, Ar3 or C1-4alkyl; R5 represents hydrogen, C1-4alkylcarbonyl- or Ar4-carbonyl-; R6 represents a substituent selected from the group consisting of C1.4alkyl, Ar5, Ar6-C1-4alkyl- or NR7R8; R7 and R8 are each independently selected from hydrogen, Het4 or C1-4alkyl; Het1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl, phenyl, phenyl-C1-4alkyl- and phenyl substituted with one or more halo substituents; Het4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substituents selected from the group consisting of amino, C1-4alkyl, hydroxy-C1-4alkyl-, phenyl, phenyl-Cl-4alkyl and phenyl substituted with one or more halo substituents; and Ar1, Ar2, Ar3, Ar4, Ar5 or Ar6 each independently represents phenyl optionally substituted one or where possible two or more substituents selected from halo, nitro, C1-4alkyl, hydroxy or C1-4alkyloxy-.

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 21725-69-9 is helpful to your research. SDS of cas: 21725-69-9

Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Electric Literature of 4865-84-3, Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. In a Article£¬once mentioned of 4865-84-3

AUXIN-LIKE ACTIVITY OF 1,2-BENZISOXAZOLE-3-ALKANOIC ACIDS

A series of benzisoxazole-alkanoic acids, differing in the length of the side-chain, have been synthesized and their activity tested on pea stem elongation, flax root growth and shoot regeneration from tomato cotyledon explants.All compounds had little or no effect on cell elongation or root growth, but a stimulating effect on shoot induction in vitro, thus showing that their activity, like that of 1,2-benzisoxazole acetic acid. is partly independent of the side-chain and is linked to the structure of the benzisoxazole ring. – Key words: 1,2-Benzisoxazole-3-alkanoic acids; auxin-like activity; pea stem elongation; flax root growth; in vitro shoot generation.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Reference of 16263-52-8, 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. 16263-52-8, Name is 3-Chloro-1,2-benzisoxazole, molecular formula is C7H4ClNO. In a Patent£¬once mentioned of 16263-52-8

OXINDOLE SUBSTITUTED PIPERAZINE DERIVATIVES

The invention relates to compounds of the formula (I), wherein Ar, A, R, R1, R2, R3, R4 and R5 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 21725-69-9, Name is Benzo[d]isoxazol-3-ol,introducing its new discovery., Computed Properties of C7H5NO2

FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF, MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

4865-84-3, Name is 1,2-Benzisoxazole-3-acetic Acid, belongs to Benzisoxazole compound, is a common compound. Formula: C9H7NO3In an article, once mentioned the new research about 4865-84-3.

1H-PYRROLE-2,5-DIONE COMPOUNDS AND METHODS OF USING THEM TO INDUCE SELF-RENEWAL OF STEM/PROGENITOR SUPPORTING CELLS

The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Formula: C9H7NO3, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about Formula: C9H7NO3

Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics